Note: Descriptions are shown in the official language in which they were submitted.
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TITLE
HERBICIDAL OXADIAZOLIDINES
BACKGROUND OF THE INVENTION
This invention relates to certain oxadiazolidines, processes for their
preparation, their
N oxides, agriculturally suitable salts and compositions, and methods of their
use for
controlling undesirable vegetation. This invention also relates to mixtures of
herbicides that
have a synergistic effect on weeds or have a safening effect on crops while
retaining or
increasing weed control.
The control of undesired vegetation is extremely important in achieving high
crop
efficiency. Achievement of selective control of the growth of weeds especially
in such
useful crops as rice, soybean, sugar beet, corn (maize), potato, wheat,
barley, tomato and
plantation crops, among others, is very desirable. Unchecked weed growth in
such useful
crops can cause significant reduction in productivity and thereby result in
increased costs to
the consumer. The control of undesired vegetation in noncrop areas is also
important. Many
products are commercially available for these purposes, but the need continues
for new
compounds which are more effective, less costly, less toxic, environmentally
safer or have
different modes of action. Arch. Pharm. (1974), 307, 7-12 discloses the
chemical structures
of N,N disubstituted 4-aryloxazolidindiones. However, it does not disclose the
compounds
of the present invention.
SUMMARY OF THE INVENTION
This invention is directed to compounds and processes to prepare compounds of
Formula 1 including all geometric and stereoisomers, N oxides, and
agriculturally suitable
salts thereof, agricultural compositions containing them and their use for
controlling
undesirable vegetation:
Q.--(cR6R7>q-
xl
wherein
Q is H; or C1-C12 alkyl, C3-Clp cycloalkyl, C6-C14 bicycloalkyl, C3-C12
alkenyl,
C3-Clp cycloalkenyl, C6-C14 bicycloalkenyl or C3-C12 alkynyl, each optionally
substituted with one or more R21; or
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Q is a 3- to 7-membered fully saturated or 5- to 7-membered partially
saturated
heterocyclic ring containing one or two X, provided that (a) when X is other
than
O or S(O)n, then only one X may be present and (b) when two X are present in
the ring, they cannot be bonded directly to each other; or
Q is a 5- or 6-membered aromatic heterocyclic ring system containing 1 to 3
heteroatoms independently selected from the group consisting of nitrogen,
oxygen and sulfur, provided that the heterocyclic ring system contains no more
than one oxygen and no more than one sulfur, and each heterocyclic ring system
is optionally substituted with one or more R16; and when Q is a 5- or 6-
membered aromatic heterocyclic ring system containing a nitrogen, then Q is
bonded through any available carbon or nitrogen atom by replacement of a
hydrogen on said carbon or nitrogen atom; or
Q is phenyl optionally substituted with one or more substituents independently
selected from the group consisting of R16, phenoxy and Z; or
Q is
/ / /
~12~ (R12~ ~ ~l~t I
\ \ /
Y/ Y~ \ I
or ; or
Q is -C(R14)(=NOR15), -C(O)R19, -C(O)OR19, -C(O)SR19, -C(S)R19~ _C(S)OR19~
-C(S)SR19, _C(O)I~jR23R24~ _C(S)NR23R24~ _QR19~ _j~19R20~ _s(p)nRl9 or
-S(O)nNR19R20;
each X is -O-, -S(O)n , -N=, -NR1~- or -Si(Ri 1)2-;
Y is, together with the carbons to which it is attached, a fully or partially
saturated 5-,
6- or 7-membered carbocyclic ring optionally substituted with one or more
C1-C4 alkyl groups; or
Y is, together with the carbons to which it is attached, a fully or partially
saturated 5-,
6- or 7-membered heterocyclic ring which contains one or two X and is
optionally substituted with one or more R12, provided that when said
heterocyclic ring contains two X, then one X is other than O;
Z is phenyl or a 5- or 6-membered aromatic heterocyclic ring system containing
1 to 3
heteroatoms independently selected from the group consisting of nitrogen,
oxygen and sulfur, provided that the heterocyclic ring system contains no more
than one oxygen and no more than one sulfur, and each phenyl and heterocyclic
ring system is optionally substituted with one or more R16;
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R1 is C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 alkenyl, C3-C6 haloalkenyl, C3-C6
alkynyl,
C3-C6 haloalkynyl, C1-C6 alkoxy, C2-C6 alkoxyalkyl or C2-C6 haloalkoxyalkyl;
or Rl is C3-C7 cycloalkyl or C3-C7 cycloalkenyl, each optionally substituted
with one or more R5; or
R1 is phenyl optionally substituted with one or more R13; or
Rl is a 5- or 6-membered aromatic heterocyclic ring system containing 1 to 3
heteroatoms independently selected from the group consisting of nitrogen,
oxygen and sulfur, provided that the heterocyclic ring system contains no more
than one oxygen and no more than one sulfur, and each heterocyclic ring system
is optionally substituted with one or more R16;
R2 is C1-C6 alkyl, C1-C6 haloalkyl, C3-C7 cycloalkyl, C3-C6 alkenyl, C3-C6
haloalkenyl, C3-C6 alkynyl, C3-C6 haloalkynyl, C1-C6 alkoxy, C2-C6
alkoxyalkyl, C2-C6 haloalkoxyalkyl or NR3R4; or
R2 is
-~~17R18~q W
~8~; or
Rl and R2 are taken together as -CH2CH2-, -CH2CH2CH2-, -CH2CH2CH2CH2-,
-CH2CH2CH2CH2CH2- or -CH2CH20CH2CH2-;
R3 is C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 alkenyl, C3-C6 haloalkenyl, C3-C6
alkynyl,
C3-C6 haloalkynyl; or
R3 is C3-C7 cycloalkyl or C3-C7 cycloalkenyl, each optionally substituted with
one or
more R5; or
R3 is a saturated or partially saturated 5-, 6- or 7-membered heterocyclic
ring
containing 1 to 2 heteroatoms independently selected from the group consisting
of nitrogen, oxygen and sulfur, and each heterocyclic ring is optionally
substituted with one or more RS; or
R3 is phenyl optionally substituted with one or more R26 groups; or
R1 and R3 are taken together with the two nitrogen atoms to which they are
attached to
form a saturated or partially saturated 5-, 6- or 7-membered heterocyclic ring
containing an optional third heteroatom selected from the group consisting of
oxygen, sulfur and nitrogen, and said heterocyclic ring is optionally
substituted
with one or more R9; or
R2 and R13, together with the two atoms to which they are attached and the
atom
between them, form a fully saturated 5-, 6- or 7-membered carbocyclic or
heterocyclic ring containing one oxygen, one sulfur or one or two nitrogen
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atoms, said heterocyclic ring is optionally substituted with one or more R12,
provided that when said heterocyclic ring contains two nitrogen atoms, they
are
other than bonded directly to each other;
R4 is H or C1-C4 alkyl; or
R3 and R4 are taken together with the nitrogen atom to which they are attached
to form
a saturated or partially saturated S-, 6- or 7-membered heterocyclic ring
containing an optional second heteroatom selected from the group consisting of
oxygen, sulfur and nitrogen, and said heterocyclic ring is optionally
substituted
with 1-4 R9;
each RS is independently halogen, Ci-C4 alkyl or C1-C4 alkoxy; or when two RS
are
attached to the same carbon, then said two RS groups are taken together as
(=O);
each R6 and R7 are independently H or C1-C4 alkyl;
Rg is independently C1-C4 alkyl, C1-C4 haloalkyl or C1-C4 alkoxy;
each R9 is independently C1-C4 alkyl or C1-C4 alkoxy; or when two R9 are
attached to
the same carbon, then said two R9 groups are taken together as (=O);
W is, together with the carbons to which it is attached, a fully or partially
saturated 5-,
6- or 7-membered heterocyclic ring containing one or two X, provided that (a)
when X is other than O or S(O)n, then only one X may be present; (b) when two
X are present in the ring, they cannot be bonded directly to each other; and
(c)
said heterocyclic ring is bonded to the group (CR17R18)q through other than X;
R1~ is H, C1-C4 alkyl, C1-C4 haloalkyl, C3-C4 alkenyl, C3-C4 alkynyl, C2-C4
alkoxycarbonyl or C2-C4 alkylcarbonyl; or R1~ is phenyl optionally substituted
with C1-C3 alkyl, halogen, cyano, vitro or C2-C4 alkoxycarbonyl;
each R 11 is C 1-C4 alkyl;
each R12 is independently halogen, Cl-C4 alkyl, Ci-C4 haloalkyl, C1-C4 alkoxy,
C1-C4 haloalkoxy, C1-C4 alkylthio, C1-C4 haloalkylthio, C1-C4 alkylsufinyl,
C1-C4 alkylsufonyl or C2-C4 alkoxycarbonyl;
each R13 is independently halogen, C1-C3 alkyl, C1-C3 haloalkyl, C1-C3 alkoxy,
C1-C3 haloalkoxy, C3-C6 alkenyloxy, C3-C6 alkynyloxy, C1-C4 alkylthio, C1-C4
haloalkylthio, C1-C4 alkylsufinyl, C1-C4 alkylsufonyl, cyano, amino, vitro or
C2-C4 alkoxycarbonyl;
R14 is H, C1-C6 alkyl, C1-C6 haloalkyl or C2-C6 alkoxyalkyl; or
R14 and R6, together with the carbon atoms to which they are bonded, form a 5-
or 6-
membered saturated carbocyclic ring optionally substituted with one or more
C1-C4 alkyl groups;
R15 is H, C1-C6 alkyl, C1-C6 haloalkyl, C3-C4 alkenyl or C3-C4 alkynyl;
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each R16 is independently halogen, vitro, cyano, C1-C4 alkyl, C1-C4 haloalkyl,
C3-C4
alkenyl, C3-C4 alkynyl, OR22, NR23R24 or S(O)nRl9;
each R17 and R18 are independently H or C1-C4 alkyl;
each R19 and R2~ are independently C1-C12 alkyl, C3-Cg cycloalkyl, C3-C12
alkenyl,
5 C3-Cg cycloalkenyl or C3-C12 alkynyl, each optionally substituted with one
or
more R21;
each R21 is halogen, C4-Cg trialkylsilylalkyl, CN, N02, -OR22, -NR23R24~
_S(O)nR22~
-S(O)nNR23R24~ _C(p)R22~ _C(S)1Z22~ -C(O)OR22~ -C(S)OR22~ -C(S)SR22~
_C(O)NR23R24~ _C(S)jVR23R24~ _CHRZSCOR22, -CHR25P(O)(OR22)2,
-CHR25P(S)(OR22)2, -CHR25C(O)NR23R24, _CHR25C(O)NH2,
-CHR25C02R22, phenyl optionally substituted with one or more R26 groups or
benzyl optionally substituted with one or more R26 groups;
each R22 is C1-Cg alkyl, C3-Cg cycloalkyl, C3-Cg alkenyl, C3-Cg alkynyl, C1-Cg
haloalkyl, C2-Cg alkoxyalkyl, C2-Cg alkylthioalkyl, C2-Cg alkylsulfinylalkyl,
1 S C2-Cg alkylsulfonylalkyl, C4-Cg alkoxyalkoxyalkyl, C4-Cg cycloalkylalkyl,
C4-Cg alkenoxyalkyl, C4-Cg alkynyloxyalkyl, C6-Cg cycloalkoxyalkyl, C4-Cg
alkenyloxyalkyl, C4-Cg alkynyloxyalkyl, C3-Cg haloalkoxyalkyl, C4-Cg
haloalkenoxyalkyl, C4-Cg haloalkynyloxyalkyl, C6-Cg cycloalkylthioalkyl,
C4-Cg alkenylthioalkyl, C4-Cg alkynylthioalkyl, C1-C4 alkyl substituted with
phenoxy or benzyloxy, each ring optionally substituted with halogen, C1-C3
alkyl or C1-C3 haloalkyl, C4-Cg trialkylsilylalkyl, C3-Cg cyanoalkyl, C3-Cg
halocycloalkyl, C3-Cg haloalkenyl, CS-Cg alkoxyalkenyl, CS-Cg
haloalkoxyalkenyl, CS-Cg alkylthioalkenyl, C3-Cg haloalkynyl, CS-Cg
alkoxyalkynyl, CS-Cg haloalkoxyalkynyl, CS-Cg alkylthioalkynyl, C2-Cg alkyl
carbonyl, C2-Cg alkoxy carbonyl, phenyl optionally substituted with halogen,
CN, C1-C2 haloalkyl and C1-C2 haloalkoxy or benzyl optionally substituted with
halogen, C1-C3 alkyl and C1-C3 haloallcyl;
each R23 is H or C1-C4 alkyl;
each R24 is C1-C4 alkyl or phenyl optionally substituted with one or more R26
groups;
R23 and R24 may be taken together as -(CH2)5-, -(CH2)4- or -CH2CH20CH2CH2-,
each ring optionally substituted with C1-C3 alkyl, phenyl or benzyl;
each R25 is H or C1-C4 alkyl;
each R26 is C1-C3 alkyl, C1-C3 haloalkyl, C1-C3 alkoxy, C1-C3 haloalkoxy, C1-
C3
alkylthio, C2-Cg alkylcarbonyl, C2-CS alkoxycarbonyl, halogen, amino, cyano or
vitro;
R2g is H or C1-C4 alkyl;
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X1 and X2 are independently O or S;
X3 is O, S or NR2g;
m is 0, 1, 2, 3 or 4;
each n is independently 0, 1 or 2;
pis0orl;
each q is independently 0, 1 or 2; and
t is 0, 1 or 2;
provided that when Q is unsubstituted phenyl, X1, X2 and X3 are O, q is 0 and
R2 is
methyl, then R1 is other than methyl.
In the above recitations, the term "alkyl", used either alone or in compound
words such
as "alkylthio" or "haloalkyl" includes straight-chain or branched alkyl, such
as, methyl,
ethyl, n-propyl, i-propyl, or the different butyl, pentyl or hexyl isomers.
The term "1-2
alkyl" indicates that one or two of the available positions for that
substituent may be alkyl.
"Alkenyl" includes straight-chain or branched alkenes such as 1-propenyl, 2-
propenyl, and
the different butenyl, pentenyl and hexenyl isomers. "Alkenyl" also includes
polyenes such
as 1,2-propadienyl and 2,4-hexadienyl. "Alkynyl" includes straight-chain or
branched
alkynes such as 1-propynyl, 2-propynyl and the different butynyl, pentynyl and
hexynyl
isomers. "Alkynyl" can also include moieties comprised of multiple triple
bonds such as
2,5-hexadiynyl. "Alkoxy" includes, for example, methoxy, ethoxy, n-propyloxy,
isopropyloxy and the different butoxy, pentoxy and hexyloxy isomers.
"Alkoxyalkyl"
denotes alkoxy substitution on alkyl. Examples of "alkoxyalkyl" include
CH30CH2,
CH30CH2CH2, CH3CH20CH2, CH3CH2CH2CH20CH2 and CH3CH20CH2CH2.
"Alkylthio" includes branched or straight-chain alkylthio moieties such as
methylthio,
ethylthio, and the different propylthio, butylthio, pentylthio and hexylthio
isomers.
"Cycloalkyl" includes, for example, cyclopropyl, cyclobutyl, cyclopentyl and
cyclohexyl.
"Saturated Carbocyclic" ring denotes a ring having a backbone consisting of
carbon atoms
linked to one another by single bonds; unless otherwise specified, the
remaining carbon
valences are occupied by hydrogen atoms.
The term "halogen", either alone or in compound words such as "haloalkyl",
includes
fluorine, chlorine, bromine or iodine. Further, when used in compound words
such as
"haloalkyl", said alkyl may be partially or fully substituted with halogen
atoms which may
be the same or different. Examples of "haloalkyl" include F3C, C1CH2, CF3CH2
and
CF3CC12. The terms "haloalkenyl", "haloalkynyl", "haloalkoxy", and the like,
are defined
analogously to the term "haloalkyl". Examples of "haloa.lkenyl" include
(Cl)2C=CHCH2
and CF3CH2CH=CHCH2. Examples of "haloalkynyl" include HC--__CCHCI, CF3C-C,
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CC13C---C and FCHZC--__CCH2. Examples of "haloalkoxy" include CF30, CC13CH20,
HCF2CH2CH20 and CF3CH20.
The total number of carbon atoms in a substituent group is indicated by the
"Ci-Cj"
prefix where i and j are numbers from 1 to 12. For example, C1-C3
alkylsulfonyl designates
methylsulfonyl through propylsulfonyl; C2 alkoxyalkyl designates CH30CH2; C3
alkoxyalkyl designates, for example, CH3CH(OCH3), CH30CHZCH2 or CH3CH20CH2;
and C4 alkoxyalkyl designates the various isomers of an alkyl group
substituted with an
alkoxy group containing a total of four carbon atoms, examples including
CH3CH2CH20CH2 and CH3CHZOCH2CH2. In the above recitations, when a compound of
Formula 1 contains a heterocyclic ring, all substituents are attached to this
ring through any
available carbon or nitrogen by replacement of a hydrogen on said carbon or
nitrogen.
When a group contains a substituent which can be hydrogen, for example R3,
then,
when this substituent is taken as hydrogen, it is recognized that this is
equivalent to said
group being unsubstituted.
Compounds of this invention can exist as one or more stereoisomers. The
various
stereoisomers include enantiomers, diastereomers, atropisomers and geometric
isomers. One
skilled in the art will appreciate that one stereoisomer may be more active
and/or may
exhibit beneficial effects when enriched relative to the other stereoisomer(s)
or when
separated from the other stereoisomer(s). Additionally, the skilled artisan
knows how to
separate, enrich, and/or to selectively prepare said stereoisomers.
Accordingly, the present
invention comprises compounds selected from Formula 1, N oxides and
agriculturally
suitable salts thereof. The compounds of the invention may be present as a
mixture of
stereoisomers, individual stereoisomers, or as an optically active form.
One skilled in the art will appreciate that not all nitrogen containing
heterocycles can
form N oxides since the nitrogen requires an available lone pair for oxidation
to the oxide;
one skilled in the art will recognize those nitrogen containing heterocycles
which can form
N oxides. One skilled in the art will also recognize that tertiary amines can
form N oxides.
Synthetic methods for the preparation of N oxides of heterocycles and tertiary
amines are
very well known by one skilled in the art including the oxidation of
heterocycles and tertiary
amines with peroxy acids such as peracetic and m-chloroperbenzoic acid
(MCPBA),
hydrogen peroxide, alkyl hydroperoxides such as t-butyl hydroperoxide, sodium
perborate,
and dioxiranes such as dimethydioxirane. These methods for the preparation of
N oxides
have been extensively described and reviewed in the literature, see for
example:
T. L. Gilchrist in Comprehensive Organic Synthesis, vol. 7, pp 748-750, S. V.
Ley, Ed.,
Pergamon Press; M. Tisler and B. Stanovnik in Comprehensive Heterocyclic
Chemistry, vol.
3, pp 18-20, A. J. Boulton and A. McKillop, Eds., Pergamon Press; M. R.
Grimmett and
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B. R. T. Keene in Advances in Heterocyclic Chemistry, vol. 43, pp 149-161, A.
R. Katritzky,
Ed., Academic Press; M. Tisler and B. Stanovnik in Advances in Heterocyclic
Chemistry,
vol. 9, pp 285-291, A. R. Katritzky and A. J. Boulton, Eds., Academic Press;
and
G. W. H. Cheeseman and E. S. G. Werstiuk in Advances in Heterocyclic
Chemistry, vol. 22,
pp 390-392, A. R. Katritzky and A. J. Boulton, Eds., Academic Press.
The salts of the compounds of the invention include acid-addition salts with
inorganic or
organic acids such as hydrobromic, hydrochloric, nitric, phosphoric, sulfuric,
acetic, butyric,
fumaric, lactic, malefic, malonic, oxalic, propionic, salicylic, tartaric, 4-
toluenesulfonic or
valeric acids.
Preferred compounds for reasons of better activity and/or ease of synthesis
are:
Preferred 1. Compounds of Formula 1 wherein
Q is H; or C1-C12 alkyl, C3-Cg cycloalkyl, C3-C12 alkenyl, C3-Cg cycloalkenyl
or
C3-C12 alkynyl, each optionally substituted with one or more R21; or
Q is a 3- to 7-membered fully saturated or S- to 7-membered partially
saturated
heterocyclic ring containing one or two X, provided that (a) when X is other
than
O or S(O)n, then only one X may be present and (b) when two X are present in
the ring, they cannot be bonded directly to each other; or
Q is a 5- or 6-membered aromatic heterocyclic ring system containing 1 to 3
heteroatoms independently selected from the group consisting of nitrogen,
oxygen and sulfur, provided that the heterocyclic ring system contains no more
than one oxygen and no more than one sulfur, and each heterocyclic ring system
is optionally substituted with one or more R16; and when Q is a 5- or 6-
membered aromatic heterocyclic ring system containing a nitrogen, then Q is
bonded through any available carbon or nitrogen atom by replacement of a
hydrogen on said carbon or nitrogen atom; or
Q is phenyl optionally substituted with one or more substituents independently
selected from the group consisting of R16, phenoxy and Z.
Preferred 2. Compounds of Preferred 1 wherein
Q is C1-C12 alkyl, C3-Cg cycloalkyl, C3-C12 alkenyl, C3-Cg cycloalkenyl or
C3-C12 alkynyl, each optionally substituted with one or more R21.
Preferred 3. Compounds of Preferred 1 wherein
Q is a 3- to 7-membered fully saturated or 5- to 7-membered partially
saturated heterocyclic ring containing one or two X, provided that (a)
when X is other than O or S(O)n, then only one X may be present and
(b) when two X are present in the ring, they cannot be bonded directly
to each other; or
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Q is a S- or 6-membered aromatic heterocyclic ring system containing 1 to 3
heteroatoms independently selected from the group consisting of
nitrogen, oxygen and sulfur, provided that the heterocyclic ring system
contains no more than one oxygen and no more than one sulfur, and
each heterocyclic ring system is optionally substituted with one or more
Ri6; and when Q is a 5- or 6-membered aromatic heterocyclic ring
system containing a nitrogen, then Q is bonded through any available
carbon or nitrogen atom by replacement of a hydrogen on said carbon or
nitrogen atom.
Preferred 4. Compounds of Preferred 1 wherein
Q is phenyl optionally substituted with one or more substituents independently
selected from the group consisting of R16, phenoxy and Z.
Preferred 5. Compounds of Preferred 2 wherein
Q is C1-C6 alkyl optionally substituted with one or more R21, CS-C7
cycloalkyl, C3-C7 alkenyl or C3-C6 alkynyl.
Preferred 6. Compounds of Preferred 3 wherein
Q is a 5- or 6-membered aromatic heterocyclic ring system containing 1 to 3
heteroatoms independently selected from the group consisting of
nitrogen, oxygen and sulfur, provided that the heterocyclic ring system
contains no more than one oxygen and no more than one sulfur, and
each heterocyclic ring system is optionally substituted with one or more
R16; and when Q is a 5- or 6-membered aromatic heterocyclic ring
system containing a nitrogen, then Q is bonded through any available
carbon or nitrogen atom by replacement of a hydrogen on said carbon or
nitrogen atom.
Preferred 7. Compounds of Preferred 4 wherein
Q is phenyl optionally substituted with one or more substituents
independently selected from the group consisting of R16,
Preferred 8. Compounds of Preferred 2, Preferred 3 or Preferred 4 wherein X1,
X2 and
X3 are O.
Preferred 9. Compounds of Preferred 7 wherein
Q is phenyl with substituents on the 2-, and 6-position independently selected
from the group consisting of R16
Preferred 10. Compounds of Preferred 5 wherein
qis0orl.
Preferred 11. Compounds of Preferred 6 wherein
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qis0orl.
Preferred 12. Compounds of Preferred 7 wherein
qis0orl.
Preferred 13. Compounds of Preferred 1 wherein
5 Ri is phenyl substituted with one or more R13,
Preferred 14. Compounds of Preferred 1 wherein
R2 is CZ-C6 alkyl, C2-C6 haloalkyl or C2-C6 alkoxyalkyl.
Most preferred is the compound of Formula 1 which is selected from the group
consisting of
10 (a) N (4-fluorophenyl)-N (1-methylethyl)-4-(2-methylphenyl)-3,5-dioxo-
1,2,4-oxadiazolidine-2-carboxamide;
(b) 4-(2,6-dimethylphenyl)-N (4-fluorophenyl)-N (1-methylethyl)-3,5-dioxo-
1,2,4-oxadiazolidine-2-carboxamide;
(c) 4-(2,6-dimethylphenyl)-N (1-methylethyl)-3,5-dioxo-N phenyl-1,2,4-
1 S oxadiazolidine-2-carboxamide;
(d) 4-cyclohexyl-N (1-methylethyl)-3,5-dioxo-N phenyl-1,2,4-oxadiazolidine-
2-carboxamide;
(e) 4-cyclohexyl-N (4-fluorophenyl)-N (1-methylethyl)-3,5-dioxo-1,2,4-
oxadiazolidine-2-carboxamide;
(f) N,4-bis(1-methylethyl)-3,5-dioxo-N phenyl-1,2,4-oxadiazolidine-2-
carboxamide;
(g) N (4-fluorophenyl)-N ( 1-methylethyl)-3,5-dioxo-4-(cyclopropyl)-1,2,4-
oxadiazolidine-2-carboxamide; and
(h) N (4-fluorophenyl)-N,4-bis(1-methylethyl)-3,5-dioxo-1,2,4-
oxadiazolidine-carboxamide.
The oxadiazolidines of Formula 1 are useful as herbicides. The present
invention
also relates to processes for preparing an oxadiazolidine of Formula 1. The
present
processes for preparing the oxadiazolidines of Formula 1 provided herein are
characterized
by employing a process sequence selected from process sequences A, B, C, D or
E as
described below.
PROCESS SEQUENCE A
A process for preparing a compound of Formula 1
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X2 X3
~~N,ltl
~-(~~7)q-N/ '~NN''
O R2
X1
1
wherein Q, R6, R7, q, X1, X2, X3, R1 and R2 are as defined above, comprising:
(a) contacting a compound of Formula 5
H X2R27
\~
X1~0/N
5 wherein R27 is -(CR6R7)q Q, with a compound of Formula 4
Q- (CR6R7)q- X4
4
wherein X4 is halogen or mesylate, in the presence of a base to provide a
compound of
Formula 3
R~X2
~N
Q° (~~7)q-N\
~O
3 X /l1
and
(b) contacting the compound of Formula 3 with a carbamoyl or thiocarbamoyl
chloride of Formula 2
R~
r,~C1
R2~ 2
PROCESS SEQUENCE B
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A process for preparing a compound of Formula 1
1
Q-(CR6R7)q
X1
1
wherein Q, R6, R7, q, Xi, X2, X3, R1 and R2 are as defined above, comprising:
(a) contacting a compound of Formula 5
Xl O~
5
wherein 827 is -(CR6R7)q Q, with an alcohol of Formula 6
Q- (CR6R7)q- OH
6
under reaction conditions involving a tertiary phosphine and an azo compound
to provide a
compound of Formula 3
827X2
~N
Q-(~~7)q-N\
~O
3 x //l
and
(b) contacting the compound of Formula 3 with a carbamoyl or thiocarbamoyl
chloride of Formula 2
H X2827
\~
/~' N
R; X3
~CI
R2~ 2
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PROCESS SEQUENCE C
A process for preparing a compound of Formula 1
X2 X3
~~~R1
Q- (CR6R7)q-N/\
O R2
X1
1
wherein Q, R6, R7, q, X1, X2, X3, R1 and R2 are as defined above, comprising:
(a) contacting a compound of Formula S
H X2827
X1~0/N
5
wherein 827 is -(CR6R7)q Q, with a carbamoyl or thiocarbamoyl chloride of
Formula 2
R\ X3
~CI
R2~ 2
in the presence of a base to provide the compound of Formula 1
R27-
X1 1
directly or a compound of Formula 7
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14
X2 X3
Rl
H- N
O R2
X1
and
(b) contacting the compound of Formula 7 with an alcohol of Formula 6
Q- (CR6R7)q- OH
6
S under reaction conditions involving a tertiary phosphine and an azo compound
or with a
compound of Formula 4
Q- (CR6R7)q - X4
4
in the presence of a base.
PROCESS SEQUENCE D
A process for preparing a compound of Formula 1
X2 X3
~~N'~Rl
Q° (~~7)q° N
O R2
X1
wherein Q, R6, R7, q, X2, X3, R1 and RZ are as defined above, and X1 is O,
comprising:
(a) contacting a compound of Formula 19
H
Q- (CR6R7)q°
.~ ORl
X1
19
with phosgene or thiophosgene to provide a compound of Formula 20
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X2
Q- (CR6R7)q-
ORl
X1
(b) contacting the compound of Formula 20 with hydroxylamine, following by
treatment with a base, and then an acid, to provide a compound of Formula 8
2
Q-(CR6R7)q-N ,I~qH
O
8 X
and
5 (c) contacting the compound of Formula 8 with a compound of Formula 2
R1 X3
\~C!
R2~ 2
PROCESS SEQUENCE E
10 A process for preparing a compound of Formula 1
1
Q- (CR6R7)q
X1
1
wherein Q, R6, R7, q, X1, X2, X3, R1 and R2 are as defined above, comprising:
(a) contacting a compound of Formula 2
R~
r~~C1
R2~ 2
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16
with hydroxylamine in the presence of a base to provide a compound of Formula
22
X3
Ri~ ~ ~ OH
R2 H
22
(b) contacting the compound of Formula 22 with a compound of Formula 23
xi
~- ~C-N- C= X2
23
S in the presence of a base to provide a compound of Formula 7
X2 X3
R1
H° N
O R2
Xi
and
(c) contacting the compound of Formula 7 with an alcohol of Formula 6
Q- (CR6R7)q- OH
6
under reaction conditions involving a tertiary phosphine and an azo compound
or with a
compound of Formula 4
Q- (CR6R7)q- X4
4
in the presence of a base.
PROCESS SEQUENCE F
A process for preparing a compound of Formula 1
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17
Q- (CR6R7)q-
X1
1
wherein Q, R6, R7, q, X1, X2, X3, R1 and R2 are as defined above, comprising
contacting a
compound of Formula 7
X2 X3
R1
~O R
X1
7
with an orthoformate of Formula 24
(R270)3~
24
wherein R27 is -(CR6R7)q Q, in the presence of a base.
PROCESS SEQUENCE G
A process for preparing a compound of Formula 1
X2 X3
~~N'~Rl
Q-(~~7)q-N
O R2
X1
1
wherein Q, R6, R7, q, X1, X2, X3, R1 and R2 are as defined above, comprising:
(a) contacting a compound of Formula 8
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X2
~~H
Q (CR6R7)q N/
~O
X //1
8
with a compound of Formula 26
X3
C1~ CI
26
to provide a compound of Formula 25
or a compound of Formula 27
X2 X3
_ _
Q (CR6R7)q N
~O
X1
X2 X3 X2
_ _ ~ - 7 _
Q (CR6R7)q N ~ ~ ~N ~~~ ~4 Q
O O
~~X1
X1
27
in the presence of a catalyst such as hexamethylguanidinium chloride; and
(b) contacting the compound of Formula 25 or Formula 27 with an amine of
Formula
10 13
R1
NH
R2/
13
in the presence of a base.
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19
The present invention also relates to an intermediate compound of Formula 5
H X2R~
N
Xl~ Oi N
wherein
R27 is -(CR6R7)q Q; R6, R7, q, Q, X1 and X2 are as defined above for Formula
1;
5 provided that when X1 and X2 are O and q is 0, then Q is other than
unsubstituted
benzyl. The present invention also relates to intermediate compounds of
Formula 8 and
Formula 20
2 2
X
C1
Q-(CR6R7)q-N ~ Q-(CR~'R7)q-
O ~ ORl
/ Xl
X ,
8 20
wherein
R6, R7, q, Q and X2 are as defined above for Formula 1; and X1 is O;
provided that when X2 is O and q is 0, then Q is other than unsubstituted
benzyl.
The oxadiazolidines of Formula 1 can be used alone or in combination with
other
commercial pesticides. The present invention also relates to certain rare
combinations that
surprisingly give greater-than-expected or synergistic effect, or give a less-
than-additive or
safening effect on crops while retaining or increasing synergistically weed
control. The
mixtures of compounds of Formula 1 and certain sulfonylureas have now been
discovered to
synergistically control weeds. Also, the mixtures of compounds of Formula 1
and safeners
such as dichlormid or naphthalic anhydride have now been discovered to exhibit
a crop
safening effect while retaining or synergistically increasing weed control.
This invention also relates to a herbicidal composition comprising a
herbicidally
effective amount of a compound of Formula 1 and at least one of a surfactant,
a solid diluent
or a liquid diluent. The preferred compositions of the present invention are
those which
comprise the above preferred compounds.
This invention also relates to a method for controlling the growth of
undesired
vegetation comprising contacting the vegetation or its environment with a
herbicidally
effective amount of a compound of Formula 1.
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DETAILS OF THE INVENTION
Compounds of the Formula 1 can be readily prepared by one skilled in the art
by
using the reactions and techniques described in Scheme 1 to Scheme 10 below.
In cases
where a substituent of the starting material is not compatible with the
reaction conditions
5 described for any of the reaction schemes, the substituent can be converted
to a protected
form prior to the described reaction scheme and then deprotected after the
reaction using
commonly accepted protection/deprotection techniques (see Green, T. W and
Wuts, P. G.,
Protecting Groups in Organic Transformations, 2nd Edition, John Wiley and
Sons, New
York, 1991). Otherwise, alternative approaches known to one skilled in the art
are available.
10 The definitions of Q, X1, X2, X3, R1, R2, R6, R7, and q in compounds of
Formulae 1-21
below are as defined in the Summary of the Invention.
As shown in Scheme 1, compounds of Formula 1 can be obtained by the reaction
of
oxadiazolidines of Formula 8 with carbamyl chlorides of Formula 2. The
preferred solvent
for the carbamoylation reaction is an inert solvent such as tetrahydrofuran,
toluene, benzene
1 S or dioxane. The presence of a tertiary amine base such as triethylamine or
diisopropylethylamine is preferable. Use of an acylation catalyst such as
4-dimethylaminopyridine or 4-pyrrolidinopyridine in a catalytic or
stoichiometric amount is
preferred. Other bases such as alkali hydroxide, carbonates or hydrides may
also be
employed. The reaction can be carried out at temperatures between 20 to 150
°C.
SCHEME 1
X2 X3 X2 X3
~ R1
NH R1 Base 7 - ~ N' _ N'
Q- (CR6R xl N ~ + w N~ ~ --s Q- (C~6R ) N
O ~2 q ~O R2
//R
Xl X1
2
Oxadiazolidines of Formula 8 can be prepared by methods known in the
literature.
Zinner reported the preparation of a wide variety of oxadiazolidines. See, for
example:
Arch. Pharm. (1965), 298, 580-587; Arch. Pharm. (1971), 303, 139-144, German
patent
application, DE 2010396 (1971). As shown in Scheme 2, a hydroxyurea or
hydroxythiourea
of Formula 9 is reacted with an activated carbonyl or thiocarbonyl compound of
Formula 10
in the presence of a base to give compounds of Formula 8. Examples of suitable
activated
carbonyl compounds are ethyl chloroformate, phenyl chlorofonmate, carbonyl
diimidazole,
phosgene, diphosgene or triphosgene. Examples of suitable activated
thiocarbonyl
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21
compounds are carbon disulfide, thiophosgene and thiocarbonyldiimidazole.
Suitable bases
include alkali carbonates, tertiary amines such as triethylamine and alkali
hydroxides. The
reaction can be carried out in a variety of solvents including
tetrahydrofuran, toluene,
dichloromethane, chloroform, acetonitrile or dioxane. The reaction may also be
carried out
in two-phase mixtures of water and an organic solvent such as dichloromethane,
ethyl
acetate or toluene. Depending on the reactivity of the carbonyl or
thiocarbonyl compound,
the reaction may be carried out at temperatures from 0 to 150 °C.
SCHEME 2
X2 X1
Q°(~~7)q~~~OH + M~M2 B~ 8
H H
9 10
M l, M2 is halogen, phenoxy, OCH3, OC2H5 or imidazole
As shown in Scheme 3, compounds of Formula 8a wherein Xl and X2 are O can be
made via the method of Zinner, Arch. Pharm. (1981), 314, 294-302. The reaction
of
isocyanates of Formula 11 with hydroxyurethanes of Formula 12 gives compounds
of
Formula 8a. The cyclization can be carried out in a variety of solvents such
as acetone,
dichloromethane, tetrahydrofuran, dioxane, ethyl acetate, and other solvents
inert to
isocyanates. The presence of a base such as triethylamine or sodium hydroxide
is also
useful. The reaction may be carried out at temperatures from 20 to 150
°C.
SCHEME 3
X2
HO COOR
Q- (~6R7)q- N~2 + ~ ~ .~ ~ (~6R7)q_ N IfVH
H ~O
11 12 X1
(R is alkyl, allyl or aryl) 8a (wherein X1 and XZ are O)
Carbamyl chlorides of Formula 2a (which are compounds of Formula 2 wherein X3
is O) are well known in the literature and can be made by the reaction of
amines of Formula
13 with phosgene or a phosgene equivalent such as di- or triphosgene as shown
in Scheme 4.
The presence of a base is useful and the use of hindered tertiary amines such
as
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22
diisopropylethyl amine is preferred. The reaction can be carried out in a
variety of solvents
such as toluene or benzene that are inert to phosgene and its equivalents. The
reaction can
be carned out at temperatures from 0 to 120 °C.
SCHEME 4
Phosgene O
or 1
\ ~ equivalent R \ ~ ~
R2~ Base R2
13 2a
As shown in Scheme 5, hydroxyureas and thioureas of Formula 9 can be prepared
from the reaction of hydroxylamine with isocyanates or isothiocyanates of
Formula 11. The
reaction is carried out in a two-phase reaction medium consisting of water and
an organic
solvent such as toluene, benzene, dichloroethane, dichloromethane, ethyl
acetate or
chlorobutane. The hydroxylamine employed can be a commercially available
aqueous
solution or can be prepared in situ from the reaction of an acid addition salt
of
hydroxylamine with an alkali hydroxide or carbonate. The reaction is generally
carried out
at temperatures between 0 and 40 °C.
SCHEME 5
X2
Q-(CR6R7)q-NCX2 ~2~ Q-(CR6R7)q\~N/0H
H H
11 9
Isocyanates of Formula 11 a are commercially available or can be prepared from
amines of Formula 14 as shown in Scheme 6. The reaction of phosgene or its
equivalents
(such as di- and triphosgene) with amines or amine hydrochlorides of Formula
14 gives the
isocyanates of Formula 11 a. This reaction is well known in the literature and
can be carried
out in a variety of solvents such as toluene, benzene, ethyl acetate or
dichloroethane which
are inert to phosgene. Depending upon the reactivity of the amine of Formula
14, the
reaction may be carried out at temperatures from 0 to 200 °C.
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23
SCHEME 6
Phosgene
or
equivalent
Q- (CR6R7)q- NH2 --~ Q- (CR6R7)q- N= ~ X2
14 11 a (wherein X2 is O)
As shown in Scheme 7, isocyanates of Formula 11 a can also be formed from
activated acids of Formula 15. Acid halides, anhydrides, imidazolides and the
like can be
reacted with various azides to provide, after a Curtius rearrangement, the
isocyanates of
Formula 11 a. The azide used may be an alkali azide, trialkylsilyl azide or
trialkylstannyl
azide. The reaction may be carried out in solvents such as toluene,
tetrahydrofuran, ethyl
acetate, dioxane, benzene, or methyl tent-butyl ether. When an alkali azide is
employed,
biphasic aqueous solvents or miscible aqueous containing mixtures are
preferred in the
formation of the acyl azide intermediate. For further examples of Curtius
rearrangements,
see: March, J. Advanced Organic Chemistry, 3rd edition; John Wiley & Sons,
1985; pp 984-
985 and 380. See also Kim, World Patent Application 98/51683 (1998) and
Larock,
Comprehensive Organic Transformations, VCH, 1989, pp 931-932.
SCHEME 7
Q- (~~7)q ° COT -~ Q- (CR6R7)q- N= ~ X2
11 a (wherein X2 is O)
T is halogen, imidazole, etc.
M is allcali metal, tiiallcylsilyl or trialkylstannyl
15 As shown in Scheme 8, compounds of Formula 9 can also be made by the
reaction of
compounds of Formula 16 with hydroxylamine. The reaction may be carried out in
a
number of different solvents including tetrahydrofuran, dioxane, acetonitrile,
dimethylformamide and dimethylsulfoxide. Temperatures from 0 to 160 °C
may be
employed in this transformation. Many compounds of Formula 16 are known, and
can be
made by the reaction of commercially available chloroformates and
chlorothioformates with
compounds of Formula 14.
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24
SCHEME 8
w
X2 / I
Q- (~~7)q w ~ ~ ~~H s 9
N' _ O
H
16
(W is H, halogen or NO~
As shown in Scheme 9, compounds of Formula 9 can also be made by the reaction
of
activated hydroxylamines of Formula 17 with amines of Formula 14. The reaction
may be
carned out in a number of different solvents including tetrahydrofuran,
dioxane, acetonitrile,
dimethylformamide and dimethylsulfoxide. In some cases lower alcohols or even
mixtures
of water and alcohols may also be employed. Temperatures from 0 to 160
°C may be
employed in this transformation. Compounds of Formula 17 are known in the
literature and
can be made from hydroxylamine and activated esters or thioesters (See Oesper
and Broker,
J. Am. Chem. Soc., 1925, 47, 2607; Defoin et. al., Helv. Chim. Acta., 1992,
75, 109-123; and
Stewart and Brooks, J. Org. Chem., 1992, 57, 5020-5023).
SCHEME 9
w
X2
14 + ~
i
17
(W is H, halogen orNO~
Compounds of Formula 2b (which are compounds of Formula 2 wherein X3 is
X23) c~ be made by the chlorination of areas of Formula 18 as shown in Scheme
10. The
chlorination may be carried out with a wide variety of reagents such as
phosphorus
oxychloride, thionyl chloride, phosphorous pentachloride, or
triphenylphosphine reagents
with carbon tetrachloride or chlorine. A variety of solvents may be used
including
halogenated solvents such as dichloromethane, dichloroethane, or
trichloroethane. A
preferred solvent of the transformation is dimethylformamide. The reaction may
be carned
out from 0 to 150 °C. Some known chloroamidine compounds and their
synthesis may be
found in Reid, Chem. Ber., 1975,108, 2290-2299.; Kuehle et al.; Angew. Chem.;
1969; 81;
18; and Shevchenko,V.I. et al.; J. Gen. Chem. USSR (Engl.Transl.); 1976; 46;
535-539.
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SCHEME 10
O
Chlorinating
R~ ~ Agent R~ /
NR1R2 \ ~ NR1R2
H
18 2b
Wherein X3 is NR~
Many isothiocyanates of Formula 11 a are commercially available. Amines of
Formula 13 are commercially available or can be prepared by methods disclosed
in the
5 literature. See the following references and references cited therein for
synthesis of these
materials: Kim, World Patent Application 98/51683 ( 1998); Dhar, World Patent
Application
98/35961 (1998); Rorer, World Patent Application 98/25912 (1998); and Morita
et. al.,
World Patent Application WO 98/11079 (1998).
Amines of Formula 14 are commercially available or can be synthesized by
methods
10 known in the art. See the following references and references cited therein
for synthesis of
these materials: Kim, World Patent Application 98/51683 ( 1998); Dhar, World
Patent
Application 98/35961 ( 1998); Rorer, World Patent Application 98/25912 (
1998), Goto et. al.,
European Patent Application EP 695748 (1996); Goto et. al., European Patent
Application
EP 771,797 (1997); and Goto et. al. US patent 5,589,439 (1996).
15 Activated carboxylic acids of Formula 10 are commercially available or can
be
prepared by methods disclosed in the literature. See the following references
and references
cited therein for the synthesis of these materials: Kim, World Patent
Application 98/51683
(1998); Dhar, World Patent Application 98/35961(1998); Rorer World Patent
Application
98/25912 (1998); and Goto et. al., European Patent Application EP 695748
(1996). See also
20 Larock, Comprehensive Organic Transformations, VCH, 1989, p 821 for a list
of
comprehensive references for the synthesis and chemistry of carboxylic acids
and activated
derivatives.
This invention is further directed to processes for the preparation of
compounds of
Formula 1 using process sequences described below.
30
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26
PROCESS SEQUENCE A
STEP 1
x2827 Q- (CR6R7)q \ X2827
N--
N \
X1 ~ N + Q- (~~7)q-~ ~ 1 N
O Solvent x
O
4 3
Step 1 forms compounds of Formula 3 by contacting compounds of Formula 5 with
compounds of Formula 4 in the presence of a suitable base either neat or in a
suitable
solvent.
Compounds of Formula 5 may be prepared, for example, by methods described in
Synthesis, 1991, 265.
For Step 1, the reaction temperature is generally from -10 to 250 °C,
preferably from
0 to 100 °C. The reaction times are generally from 0.25 to 48 h,
preferably from 0.25 to 24
h. Generally, the pressure is in the range of 1.013 x 102 to 2.026 x 102 KPa,
preferably
ambient pressure. Suitable solvents include typical organic solvents in which
the reactants
can be dissolved and the process of Step 1 can proceed without interference.
Examples of
such reactants include aromatics such as benzene, toluene, xylene,
chlorobenzene and
dichlorobenzene, ethers such as dioxane and tetrahydrofuran, nitrites such as
acetonitrile and
propionitrile, ethyl acetate, dichloromethane, dichloroethane, and polar
aprotic solvents such
as dimethylformamide and dimethylsulfoxide.
Suitable bases include organic trialkylamines such as trimethylamine,
triethylamine,
diisopropylethylamine, tributylamine and the like, dimethylaniline, N,N
dimethylamino-
pyridine, N methylmorpholine, 1,8-diazabicyclo[5.4.0]undec-7-ene, 1,4-
diazabicyclo[2.2.2]octane and 1,5-diazabicyclo[4.3.0]non-5-ene. 1,8-
Diazabicyclo[5.4.0]-
undec-7-ene is a particularly useful organic base for this reaction. Inorganic
bases include,
but are not limited to, potassium carbonate, sodium carbonate, potassium
hydride, sodium
hydride, lithium carbonate and cesium carbonate.
A phase transfer catalyst can accelerate the reaction in the presence of
inorganic
bases. Phase transfer catalysts include tetraalkylammonium halides, crown
ethers,
phosphonium salts, silicon analogs of crown ethers and acyclic analogs of
crown ethers.
Particularly useful as a base is the combination of potassium carbonate and a
phase transfer
catalyst.
Generally at least an equimolar amount of the Formula 4 compound is used in
respect
to the Formula 5 compound, and preferably at least a small molar excess of the
Formula 4
compound is used. More particularly, the molar ratio of the Formula 4 compound
to the
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27
Formula 5 compound is usually in the range of 1.05:1 to 10:1. In most cases,
the molar ratio
of the Formula 5 compound to the Formula 4 compound is preferably in the range
of 1.1:1 to
1.5:1. Generally at least an equivalent of base is used in respect to the
Formula 5 compound,
and preferably at least a small equivalent excess of the base is used. More
particularly, the
ratio of the number of equivalents of base to number of moles of the Formula 5
compound is
usually in the range of 1.05:1 to 10:1. In most cases, the ratio of the number
of equivalents
of base to number of moles of the Formula 5 compound is preferably in the
range of 1.1:1 to
1.5:1. The equivalent amount of base may be similar to the molar amount of the
Formula 4
compound, but this is not necessary.
The compound of Formula 4 is preferably added to the reaction mixture
containing
the compound of Formula 5 and a base either neat or in a solvent. The reaction
temperature
is maintained during and after the addition and until the reaction reaches
completion.
Isolation of product of Step 1 can be accomplished by standard worlcup
procedures or
the resultant mixture can be used directly in Step 2.
STEP 2
X3 Q- (~7)q X2
\ ~ 1
3 + R\~ ~ N
R2~ ~ Solvent Xl~ ~ N N~ 2
O ~ R
2 x3
Step 2 forms compounds of Formula 1 from the reaction of compounds of Formula
3
with compounds of Formula 2 in the presence of a suitable base in a suitable
solvent.
For Step 2, the general and preferred reaction conditions are the same as the
ones
described above for Step 1.
Alternatively, the processes of Step 1 and 2 can be combined without isolating
product of Step 1 and preferably, the reaction conditions (e.g. temperature,
mole ratio,
reaction time etc) are balanced to achieve a high yield of compound of Formula
1.
The compound of Formula 1 can be isolated by standard procedures.
PROCESS SEQUENCE B
STEP 1
H x2827
N Mitsunobu
+ Q- (CR6R7)q- OH
X1~0/N
5 6
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Step 1 forms the compounds of Formula 3 from the reaction of compounds of
Formula 5 with compounds of Formula 6 under Mitsunobu reaction conditions
involving a
tertiary phosphine and an azo compound. One skilled in the art can find a
variety of the
tertiary phosphine and azo compounds as well as solvents useful for this
transformation in
Synthesis, 1981, l and Org. Reactions, 1992, 42, 335.
For the process of Step 1, the reaction temperature is generally from about -
40 to
250 °C, preferably from -20 to 80 °C. The reaction times are
generally from about 0.20 to
24 h, preferably from 0.5 to 12 h. Generally, the pressure is from 1.013 x 102
to 5.065 x102
KPa; preferably ambient pressure.
Generally at least an equimolar amount of the Formula 5 compound is used in
respect
to the Formula 6 compound, and preferably at least a small molar excess of the
Formula 6
compound is used. More particularly, the molar ratio of the Formula 6 compound
to the
Formula 5 compound is usually in the range of 1.05:1 to 10:1. In most cases,
the molar ratio
of the Formula 6 compound to the Formula 5 compound is preferably in the range
of 1.1:1 to
1.5:1.
Isolation of product of Step 1 can be accomplished by standard workup
procedures.
STEP 2
Compounds of Formula 1 are then obtained by the reaction of the compounds of
Formula 3 prepared in Step 1 and compounds of Formula 2 under the same
reaction
conditions as already described in Step 2 for Sequence A.
STEP 1 a
PROCESS SEQUENCE C
X2R27 X2 X3
IVY R1
+ 2 ~e -s 7
N Q- W~ )q N I I
X ~ p~ O R2
5
wherein R27 is Q- (CR6R7)q- Xl 1
Step 1 a forms the compounds of Formula 1 by contacting compounds of Forniula
5
with compounds of Formula 2 in the presence of a suitable base either neat or
in a suitable
solvent.
For the process of Step 1 a, the general and preferred reaction conditions are
the same
as the ones described above for Step 1 in Process Sequence A.
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29
A solution of compound of Formula 2 can be added to a solution/suspension of
compound of Formula 5 and a base in a solvent. Reaction temperature is
maintained during
and after the addition and until the reaction reaches completion. Isolation of
product of Step
1 a can be accomplished by standard workup procedures.
STEP lb
H X2R27 H X2
~ N~ 'N~ R2
Xl~ ~N + 2 ~ Xl~ iN NvRI
O O
X3
5 7
Step lb forms the compounds of Formula 7 from the reaction of compounds of
Formula 5 and compounds of Formula 2 in the presence of a base either neat or
in a suitable
solvent.
For the process of Step lb, the general and preferred reaction conditions are
the same
as the ones described above for Step 1 in Process Sequence A.
The product of Step lb can be isolated by standard workup procedures.
STEP 2a
7 + Q- (CR6R7)q- OH M'rtsunobu ~ 1
6
Step 2a forms the compounds of Formula 1 from the reaction of compounds of
Formula 7 and compounds of Formula 6 under Mitsunobu reaction conditions
involving a
tertiary phosphine and an azo compound. One skilled in the art can find a
variety of the
tertiary phosphine and azo compounds as well as solvents useful for this
transformation in
Synthesis, 1981, l and Org. Reactions, 1992, 42, 335.
For the process of Step 2a, the reaction temperature is generally from about
~0 to
250 °C, preferably from -20 to 80 °C. The reaction times are
generally from about 0.20 to
24 h, preferably from 0.5 to 12 h. Generally, the pressure is from 1.013 x 102
to 5.065 x102
KPa; preferably ambient pressure.
Generally at least an equimolar amount of the Formula 7 compound is used in
respect
to the Formula 6 compound, and preferably at least a small molar excess of the
Formula 6
compound is used. More particularly, the molar ratio of the Formula 6 compound
to the
Formula 7 compound is usually in the range of 1.05:1 to 10:1. In most cases,
the molar ratio
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of the Formula 7 compound to the Formula 6 compound is preferably in the range
of 1.1:1 to
1.5:1.
Isolation of product of Step 2a can be accomplished by standard workup
procedures.
S STEP 2b
7 + Q--(cR6R7)q x4 -~ 1
4
Step 2b forms compounds of Formula 1 by contacting compounds of Formula 7 with
compounds of Formula 4 in the presence of a suitable base either neat or in a
suitable
solvent.
10 For the process of Step Zb, the general and preferred reaction conditions
are similar
to the ones described above for Step 1 in Process Sequence A.
Isolation of product of Step 2b can be accomplished by standard workup
procedures.
PROCESS SEQUENCE D
15 Compounds of the Formula 8 can be readily prepared by one skilled in the
art by
using the reactions and techniques described in Steps l and 2. In cases where
a substituent
of the starting material is not compatible with the reaction conditions
described for any of
the reaction schemes, the substituent can be converted to a protected form
prior to the
described reaction scheme and then deprotected after the reaction using
commonly accepted
20 protection/deprotection techniques (see Green, T. W. and Wuts, P. G.,
Protecting Groups in
Organic Transformations, 2nd Edition, John Wiley and Sons, New York, 1991).
Otherwise,
alternative approaches known to one skilled in the art are available.
STEP 1
X2
Q- (~~7)q- ~ H 1 Base Q- (CR6R7) - ~ ~
OR Phosgene q ~ ORl
or
19 X T~Phosgene 20 X1
(wherein Xl is O)
25 Step 1 forms compounds of Formula 20 from the reaction of compounds of
Formula
19 with phosgene or thiophosgene in the presence of a base. For general
reaction conditions
for this transformation, see: U.S. Patent Number 5,602,251. Compounds of
Formula 19 are
well known in the literature. See: for example, J. Chem. Soc. Perkin I (1997),
1041.
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STEP 2
X2 2
20 Hy~- ~ -> Q-(CR6R7) - NHO l~~ Q- CR6R7 - ~NH
2. Acid ( )q O
Xl /
21 8 X
(wherein X2 is O or S and X1 is O)
Step 2 forms compounds of Formula 8 in the form of a salt by treatment of
compounds
of Formula 20 with hydroxylamine and a base. The salt is then converted to
compound of
Formula 8 by treatment with an acid.
The reaction is conducted in a suitable organic solvent such as, but not
limited to,
tetrahydrofuran, dioxane or toluene at a temperature between - 20 and 100
°C with 10-50 °C
being the preferred temperature. Hydroxylamine may be generated from one of
its salts by
use of a suitable base such as, but not limited to, potassium carbonate,
potassium hydroxide
or sodium hydroxide. Alternatively, hydroxylamine in water may be used.
Judicious use of
an appropriate co-solvent such as water or a phase transfer catalyst may be
effective in
facilitating the reaction. Further amounts of the base (vide supra) can be
added to scavenge
the HCI formed in the reaction. Alternatively, an excess amount of
hydroxylamine can be
used to achieve the same purpose.
1 S The intermediate compound of Formula 21 is not usually isolated, but
converted
directly to compounds of Formula 8 by addition of further quantities of base.
It is apparent
to one skilled in the art that salts of compounds of Formula 8 generated from
this reaction
may be used directly in the preparation of compounds of Formula 1 as described
in Scheme
1. To facilitate the transformation, it may be desirable to adjust the solvent
composition by
removal of co-solvents such as water prior to the reaction. Alternatively,
compounds of
Formula 8 may be isolated from their salts by addition of an appropriate
mineral acid such
as, but not limited to, HCI before being subjected to the reaction conditions
as described in
Scheme 1 to produce compounds of Formula 1.
PROCESS SEQUENCE E
Compounds of the Formula 7 can be readily prepared by one skilled in the art
by
using the reactions and techniques described in Steps 1 and 2. Since
hydroxylamine is
unstable upon heating, this sequence allows a safe and efficient route to the
compounds of
the Formula 7 under mild conditions.
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STEP 1
X3
R1 X3 1
Base R ~ ~ OH
R2, N Cl + NH20H --~ ~ N~
2 R2 H
22
Step 1 forms the compounds of Formula 22 by contacting a compound of Formula 2
with hydroxylamine in the presence of a suitable base in a suitable solvent.
Hydroxylamine
may be generated from one of its salts or hydroxylamine in water may be used.
For Step 1, the reaction temperature is generally from -10 to 150 °C,
preferably from
0 to 100 °C. The reaction times are generally from 0.10 to 24 h,
preferably from 0.10 to 2 h.
Generally, the pressure is in the range of 1.013 x 102 to 2.026 x 102 KPa;
preferably ambient
pressure. Suitable solvents include typical organic solvents in which the
reactants can be
dissolved and the process of Step 1 can proceed without interference. Examples
of such
solvents include aromatics such as benzene, toluene, xylene, chlorobenzene and
dichlorobenzene, ethers such as dioxane and tetrahydrofuran, nitrites such as
acetonitrile and
propionitrile, ethyl acetate, dichloromethane, dichloroethane, and polar
aprotic solvents such
as dimethylformamide and dimethylsulfoxide. Judicious use of an appropriate co-
solvent
such as water or a phase transfer catalyst may be effective in facilitating
the reaction.
Suitable bases include organic trialkylamines such as trimethylamine,
triethylamine,
diisopropylethylamine, tributylamine and the like, dimethylaniline, N,N
dimethylamino-
pyridine, N methylmorpholine, 1,8-diazabicyclo[5.4.0]undec-7-ene, 1,4-
diazabicyclo[2.2.2]octane and 1,5-diazabicyclo[4.3.0]non-S-ene. Trialkylamines
is a
particularly usefizl organic base for this reaction. When an excess quantity
of hydroxylamine
is employed, the excess hydroxylamine can also serve as a base. Inorganic
bases include,
but are not limited to, potassium hydroxide, sodium hydroxide, potassium
carbonate, sodium
carbonate, lithium carbonate and cesium carbonate.
Generally at least an equimolar amount of the Formula 2 compound is used in
respect
to hydroxylamine, and preferably at least a small molar excess of
hydroxylamine is used.
More particularly, the molar ratio of the Formula 2 compound to hydroxylamine
is usually in
the range of 1:1.05 to 1:10. In most cases, the molar ratio of the Formula 2
compound to
hydroxylamine is preferably in the range of 1:1.1 to 1:1.5. Generally at least
an equivalent
of base is used in respect to the Formula 2 compound, and preferably at least
a small
equivalent excess of the base is used. More particularly, the ratio of the
number of
equivalents of base to number of moles of the Formula 2 compound is usually in
the range of
1.05:1 to 10:1. In most cases, the ratio of the number of equivalents of base
to number of
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33
moles of the Formula 2 compound is preferably in the range of 1.1:1 to 1.5:1.
The
equivalent amount of base may be similar to the molar amount of the Formula 2
compound,
but this is not necessary.
Isolation of product of Step 1 can be accomplished by standard workup
procedures.
In the scenario that the reaction is carnied our in an aqueous solution, a
filtration can be
employed to collect compounds of Formula 22.
STEP 2
xl
22 + C1- ~C- N= C= X2 -~ 7
23
Compounds of Formula 7 are synthesized by contacting compounds of Formula 22
with chlorocarbonyl isocyanate (X1 and X2 are O) or chlorocarbonyl
isothiocyanate (X1 is O
and X2 is S) or chlorothiocarbonyl isocyanate (X1 is S and X2 is O) or
chlorothiocarbonyl
isothiocyanate (X1 and X2 are S) in the presence of a base to scavange the HCl
byproduct.
Similar examples of such reactions using N alkyl-N hydroxylamine and
chlorocarbonyl
isocyanate have been reported in Syn., 1982, 781-2 and in WO 9741097 but there
is no
example of compound like 22 and chlorocarbonyl isocyanate in the literature.
Compounds of Formula 23 are either commercially available or may be prepared
by
one skilled in the art using methods known in the art (or slight modification
of these
methods); for example, see: Chem. Ber. 1981,114, 1746-S1, Chem. Ber. 1973,106,
1487-95,
and Chem. Ber. 1966, 99, 3572-81.
For Step 2, the reaction temperature is generally from -10 to 150 °C,
preferably from
0 to 100 °C. The reaction times are generally from 0.10 to 24 h,
preferably from 0.10 to 2 h.
Generally, the pressure is in the range of 1.013 x 102 to 2.026 x 102 KPa;
preferably ambient
pressure. Suitable solvents include typical organic solvents in which the
reactants can be
dissolved and the process of Step 1 can proceed without interference. Examples
of such
reactants include aromatics such as benzene, toluene, xylene, chlorobenzene
and
dichlorobenzene, ethers such as dioxane and tetrahydrofuran, nitrites such as
acetonitrile and
propionitrile, ethyl acetate, dichloromethane, dichloroethane, and polar
aprotic solvents such
as dimethylformamide and dimethylsulfoxide.
Suitable bases for Step 2 are similar to the ones described above for Step 1.
Generally at least an equimolar amount of the Formula 22 compound is used in
respect to the Formula 23 compound, and preferably at least a small molar
excess of the
Formula 23 compound is used. More particularly, the molar ratio of the Formula
22
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34
compound to the Formula 23 compound is usually in the range of 1:1.05 to 1:10.
In most
cases, the molar ratio of the Formula 22 compound to the Formula 23 compound
is
preferably in the range of 1:1.1 to 1:1.5. Generally at least an equivalent of
base is used in
respect to the Formula 22 compound, and preferably at least a small equivalent
excess of the
S base is used. More particularly, the ratio of the number of equivalents of
base to number of
moles of the Formula 22 compound is usually in the range of 1.05:1 to 10:1. In
most cases,
the ratio of the number of equivalents of base to number of moles of the
Formula 22
compound is preferably in the range of 1.1:1 to 1.5:1. The equivalent amount
of base may
be similar to the molar amount of the Formula 22 compound, but this is not
necessary.
Isolation of product of Step 2 can be accomplished by standard workup
procedures.
Compounds 7 can be readily converted into alkali salts when treated with
potassium
carbonate or sodium carbonate in water. The salts may be useful in alkylation
reactions.
Compounds of Formula 1 are then obtained by the reaction of compounds of
Formula
7 under the same reaction conditions as already described in Step 2a/2b in
Sequence C.
PROCESS SEQUENCE F
Compounds of the Formula 1 can be readily prepared by one skilled in the art
by
using the reactions and techniques described in the scheme below.
X2 X3 X2 X3
~~NiRI ~~N~RI
H- N ~ ( + ~270)3~ -"~ Q° ~CR6R7)q- N ~
O R2 O R2
24
X1 7 X1
wherein R27 is -(CR6R7}.Q
The compounds of Formula 1 are formed by contacting a compound of Formula 7
with an orthoformate of Formula 24 either neat or in the presence of a
suitable solvent.
The reaction temperature is generally from -10 to 150 °C, preferably
from 0 to 100
°C. The reaction times are generally from 0.10 to 24 h, preferably from
0.10 to 2 h.
Generally, the pressure is in the range of 1.013 x 102 to 2.026 x 102 KPa;
preferably ambient
pressure. Suitable solvents include typical organic solvents in which the
reactants can be
dissolved and the process can proceed without interference. Examples of such
reactants
include aromatics such as benzene, toluene, xylene, chlorobenzene and
dichlorobenzene,
ethers such as dioxane and tetrahydrofuran, nitrites such as acetonitrile and
propionitrile,
ethyl acetate, dichloromethane, dichloroethane, and polar aprotic solvents
such as
dimethylformamide and dimethylsulfoxide.
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Generally at least an equimolar amount of the Formula 24 compound is used in
respect to the Formula 7 compound, and preferably at least a small molar
excess of Formula
24 compound is used. More particularly, the molar ratio of the Formula 7
compound to the
Formula 24 compound is usually in the range of 1:1.05 to 1:10. In most cases,
the molar
5 ratio of the Formula 7 compound to the Formula 24 compound is preferably in
the range of
1:1.1 to 1:1.5.
PROCESS SEQUENCE G
Compounds of the Formula 1 can be readily prepared by one skilled in the art
by
using the reactions and techniques described in Steps 1 and 2.
10 STEP 1
X2 X2 X3
7 ~H X3 ~N~Q
Q- CR6R - N~ + --s 7 -
( )q / Q- (~~ )9 N
C1 C7 ~ O
Xl 26 x//l
8 25
Catalyst
X2 X3 X2
7 - ~ ~ ~ N- (CR6R~) - Q
Q- (~~ )q N ~ 1- / 9
O-~-~~~0
// X1
X1
27
Step 1 forms the compounds of Formula 25 by contacting a compound of Formula 8
with a compound of Formula 26 either neat or in a suitable solvent.
For Step 1, the reaction temperature is generally from -10 to 150 °C,
preferably from
15 0 to 100 °C. The reaction times are generally from 0.10 to 24 h,
preferably from 0.10 to 2 h.
Generally, the pressure is in the range of 1.013 x 102 to 2.026 x 102 KPa;
preferably ambient
pressure. Suitable solvents include typical organic solvents in which the
reactants can be
dissolved and the process of Step 1 can proceed without interference. Examples
of such
reactants include aromatics such as benzene, toluene, xylene, chlorobenzene
and
20 dichlorobenzene, ethers such as dioxane and tetrahydrofuran, nitrites such
as acetonitrile and
propionitrile, ethyl acetate, dichloromethane and dichloroethane.
Generally at least an equimolar amount of the Formula 26 compound is used in
respect to the Formula 8 compound, and preferably at least a small molar
excess of the
Formula 26 compound is used. More particularly, the molar ratio of the Formula
8
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36
compound to the Formula 26 compound is usually in the range of 1:1.05 to 1:10.
In most
cases, the molar ratio of the Formula 8 compound to the Formula 26 compound is
preferably
in the range of 1:1.1 to 1:1.5.
In the presence of a catalyst such as hexamethylguanidinium chloride, the
reaction of
compounds of Formula 8 and compounds of Formula 26 produces compounds of
Formula
27. For general and preferred conditions, see Tet. Lett. 1987, 5823-5826.
Isolation of product of Step 1 can be accomplished by standard workup
procedures.
STEP 2
R1
25 +
2~
R ~e X2 X3
13 ~ ~ ~ R1
Q- ~CR6R7)4 - N
O R2
1
R /NH ~e Xl 1
27 + 2
R
13
Compounds of Formula 1 are synthesized by contacting compounds of either
Formula 25 or Formula 27 with amines of Formula 13 in the presence of a
suitable base in a
suitable solvent.
For Step 2, the general and preferred reaction conditions are the same as the
ones
described above for Step 1 in Process Sequence A.
One skilled in the art will recognize that, in some cases, after the
introduction of a
given reagent as it is depicted in any individual scheme, it may be necessary
to perform
additional routine synthetic steps not described in detail to complete the
synthesis of
compounds of Formula 1. One skilled in the art will also recognize that it may
be necessary
to perform a combination of the steps illustrated in the above schemes in an
order other than
that implied by the particular sequence presented to prepare the compounds of
Formula 1.
One skilled in the art will also recognize that compounds of Formula 1 and the
intermediates described herein can be subjected to various electrophilic,
nucleophilic,
radical, organometallic, oxidation, and reduction reactions to add
substituents or modify
existing substituents.
Without further elaboration, it is believed that one skilled in the art using
the
preceding description can utilize the present invention to its fullest extent.
The following
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Examples are, therefore, to be construed as merely illustrative, and not
limiting of the
disclosure in any way whatsoever. Percentages are by weight except for
chromatographic
solvent mixtures or where otherwise indicated. Parts and percentages for
chromatographic
solvent mixtures are by volume unless otherwise indicated. 1H NMR spectra are
reported in
ppm downfield from tetramethylsilane; s = singlet, d = doublet, t = triplet, q
= quartet,
m = multiplet, dd = doublet of doublets, dt = doublet of triplets, br s =
broad singlet.
EXAMPLE 1
Step A: Preparation of N (2,4-dichloropheny~-N'-hydroxyurea
A solution of 14.2 g (75 mmol) of 2,4-dichlorophenylisocyanate in 50 mL of
toluene
was added to a mixture of 8.26 g (120 mmol) of hydroxylamine hydrochloride and
4.8 g
(120 mmol) of sodium hydroxide in a two-phase solvent mixture consisting of 50
mL of
water and SO mL of toluene. The resulting mixture was stirred at 25 °C
for 30 minutes and
filtered. The solid thus obtained was washed with water and then dissolved in
200 mL of
ethyl acetate. The solution was dried over magnesium sulfate and the solvent
was removed
under reduced pressure to yield 12.7 g of the title compound of Step A as a
white solid
melting at 157-158 °C. It was used directly in the next step without
further purification.
Step B: Preparation of 4-(2 4-dichlorophenyl)-1 2 4-oxadiazolidine-3 5-dione
A solution of 4.2 g (19 mmol) of the compound of step A in tetrahydrofuran (20
mL)
was treated with carbonyldiimidazole (3.2 g, 19 mmol). The mixture was stirred
at 25 °C for
16 h. Some precipitated imidazole was filtered off and the filtrate was
concentrated under
reduced pressure. The residue was partitioned between 1N HCl (20 mL) and ethyl
acetate
(SO mL). The organic layer was dried over magnesium sulfate and concentrated
to an oil
which solidified to give 3.8 g of the title compound of Step B as a solid
melting at 104-107
°C. It was used directly for the next step without further
purification.
Step C:, Preparation of 4-fluoro-N propylbenzenamine
A 3L three neck round bottom flask equipped with a nitrogen inlet, a
thermometer, an
overhead stirrer and a solid addition funnel was charged with 250 mL acetic
acid, 50 mL
absolute ethanol and 29.5 g (0.27 mol) of 4-fluoroaniline. To this mixture was
added
acetone (23 mL, 0.31 mol) in one portion followed by the portion-wise addition
of sodium
acetate trihydrate over S min. This vigorously stirred mixture was cooled to 0
°C (dry-
ice/acetone) and 4.5 g of sodium borohydride (1.2 mol) was added portion-wise
via a solid
addition funnel over 50 min while keeping the internal temperature below 10
°C. During
this addition, acetic acid (100 mL) and absolute ethanol (SO mL) were added to
facilitate
stirring. After the addition, the mixture was allowed to warm to room
temperature, and then
stirred at ambient temperature for 12 h. Sufficient ammonium hydroxide (30%
aqueous) was
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38
added to adjust the pH to ~8 while maintaining the internal temperature below
30 °C using
an ice/water bath. The mixture was extracted with ether (4 x 400 mL). The
combined
organic layers were washed with brine, dried over MgS04, filtered, then
concentrated under
reduced pressure to give the desired product as a black/brown oil (38 g).
1H NMR: (300 MHz, CDC13) b 6.8-6.9 (t, 2H), 6.5 (m, 2H), 3.5 (m, 1H), 1.2 (d,
6H).
Step D: Preparation of 4-(fluoro~henyl)propylcarbamic chloride
A 1 L three neck round bottom flask equipped with a nitrogen inlet, a
thermometer
and two addition funnels was charged with 600 mL of toluene and 36.0 g (0.22
mol) of the
compound of Step C. This stirred mixture was cooled to 3 °C, and then
116 mL (0.22 mol)
of a 20% solution of phosgene in toluene was added dropwise over 15 min while
maintaining the temperature below 10 °C. Ten min after the addition,
diisopropyl
ethylamine (39 mL, 0.22 mol) was added dropwise over 15 min while maintaining
the
temperature below 7 °C. The reaction mixture was allowed to warm to
room temperature
and stirred for 14 hours. The resulting brown solution was flooded with CH2Cl2
(700 mL),
and then saturated NaHC03 solution. The organic layer was separated and washed
with
saturated NaHC03 solution (3 x 500 mL), dried over MgS04, and filtered. The
solvent was
removed under reduced pressure, then in vacuo, during which time the resulting
oil slowly
crystallized. This solid was triturated with hexanes to give 36 g (78%) of a
gray solid
melting at 50-55 °C.
1H NMR: (300 MHz, CDCl3) 8 7.1-7.2 (m, 4H), 4.68 (m, 1H), 1.1-1.2 (d, 6H).
Step E: Preparation of 4-(2.4-dichlorophenyl)-N y4-fluorophenyl)-N (1
methylethyl)-3.S-dioxo-1,2.4-oxadiazolidine-2-carboxamide
A solution of 0.6 g (2.4 mmol) of the compound of Step B in toluene (25 mL)
was
treated with 0.42 g ( 1.9 mmol) of the compound of Step D and 0.35 g (2.9
mmol) of 4-
dimethylaminopyridine. The resulting mixture was heated at 80 °C for 1
hour, and
subsequently diluted with 1N hydrochloric acid (20 mL) and ethyl acetate (50
mL). The
organic layer was separated and washed with saturated brine solution (30 mL).
It was then
dried over magnesium sulfate and concentrated under reduced pressure. The
residue was
subjected to column chromatography on silica gel with 85:15 hexanes-ethyl
acetate as
eluent. Appropriate fractions were combined and concentrated to give 0.32 g of
the title
compound of Step E, a compound of this invention, as an oil which solidified
on standing to
give a solid melting at 57-60 °C.
1H NMR (CDCl3) 81.22 (m, 6H), 4.7 (m, 1H), 7.04-7.17 (m, 2H), 7.2-7.3 (m, 3H),
7.39 (d, 1H), 7.58 (s, 1H).
EXAMPLE 2
Step A: Preparation of N (2.6-dimethylphenyl~-N'-hydrox~rlurea
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39
A 500 mL side arm flask equipped with a thermometer and an addition funnel
with a
nitrogen inlet was charged with 100 mL of toluene and 2.00 g (0.10 mol) of 50%
hydroxylamine in water. A solution of 4.41 g of 2,6-dimethylphenyl isocyanate
(0.03 mol)
dissolved in 50 mL of toluene was added dropwise over 15 min. External cooling
was used
to maintain the internal reaction temperature below 25 °C. Stirring was
continued at room
temp for 18 h. The solvent was removed under reduced pressure to give a white
solid. The
residual solvent was further co-evaporated twice with toluene, then oven dried
overnight to
give the desired product (5.25 g) as a white solid melting at 192-193
°C.
1H NMR: (300 MHz, DMSO-d6) 8 8.85 (d, 1H), 8.58 (s, 1H), 8.14 (s, 1H), 7.00-
7.08
(m, 3H), 2.15 (s, 6H).
Step B: Preparation of 4-(2 6-dimeth~nhenyl)-1 2 4-oxadiazolidine-3 5-dione
A 300 mL flask with side arm equipped with a nitrogen inlet and a thermometer
was
charged with 25 mL of tetrahydrofuran followed by 5.00 g (0.0277 mol) of 2,6-
dimethylphenyl hydroxyurea. To this stirred suspension was added portion-wise
4.41 g
(0.0277 mol) of carbonyl diimidazole over 5 min. While stirnng at room
temperature, the
suspension turned into a solution before precipitate started to form slowly.
After 18 h, the
mixture was quenched with 50 mL of 1N HCl which caused the suspension to turn
into a
solution. It was partitioned between ethyl acetate (250 mL) and 1N HCl (50
mL). The
organic layer was separated and washed with brine, then dried over MgS04 and
filtered.
The solvent was removed under reduced pressure to give the title compound as a
red oil
(5.20 g) which slowly crystallized upon standing at room temperature to give a
solid melting
at 90-100 °C.
1H NMR: (300 MHz, CDCl3) 8 7.30 (t, 1H), 7.20 (d, 2H), 2.24 (s, 6H).
Step C: Preparation of 4-(2,6-dimethylphenyl)-N (4-fluorophenyl)-N (1-
methylethyl)-
3.5-dioxo-1,2.4-oxadiazolidine-2-carboxamide
To a 500 mL two neck round bottom flask equipped with a thermometer and a
reflux
condenser with nitrogen inlet was charged sequentially 30 mL of toluene, 1.50
g (0.0072
mol) of the compound of Step B, 1.60 g (0.0074 mol) of the compound of Step D
in
Example 1, and lastly 0.90 g of 4-dimethylaminopyridine (0.072 mol). The
reaction became
homogeneous upon heating to 85 °C. Heating was continued at 85
°C for 2 h during which
time a precipitate was formed. The reaction mixture was then cooled to room
temperature,
filtered and the solid was washed with toluene (2 x 25 mL). The toluene was
removed under
reduced pressure to give a tan solid. The product was washed with cool
isopropyl alcohol (2
x 10 mL) to give 2.16 g of the title compound, a compound of the invention, as
a white solid
melting at 134-136 °C.
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1H NMR: (300 MHz, DMSO-d6) S 7.20-7.47 (m, 7H), 4.52-4.65 (m, 1H), 2.03
(s, 6H).
EXAMPLE 3
Step A: Preparation of 4-(2-propenyl)-1 2 4-oxadiazolidine-3 5-dione
S To a 500 mL round-bottom flask were added acetone (300 mL), allyl isocyanate
(12.0 g, 0.145 mol), N-hydroxyurethane (6.1 g, 0.058 mol) and triethylamine
(11.7 g, 0.116
mol) respectively at room temperature under nitrogen with efficient stirring.
The reaction
mixture was allowed to stir at room temperature for 6 d. The solvent was
removed under
reduced pressure. The residue was suspended in 100 mL of 1N HCI, extracted
with ethyl
10 acetate (3 x 150 mL). The organic solution was washed with water, brine,
dried over
MgS04 and concentrated to a clear yellow oil. The crude product was dried
under high
vacuum for 4 h to give the title compound as an oil (13.1 g) which was used in
the next step
without further purification.
1H NMR: (300 MHz, CDC13) 8: 5.87 (m, 1H), 5.27 (m, 2H), 4.17 (m, 1H), 3.82
1 S (bs, 1 H).
Step B: Preparation of N (4-fluorophenyl)-N ( 1-meth~yl)-3 S-dioxo-4-(2-
pronenyl)-1.2.4-oxadiazolidine-2-carboxamide
A dry 100 mL round-bottom flask was changed with dry tetrahydrofuran (20 mL),
the compound of step A (1.0 g, 7.0 mmol), the compound of Step D in Example 1
(1.5 g, 7.0
20 mmol), triethylamine (1.0 g, 10.0 mmol) and 4-dimethylaminopyridine (0.2 g,
1.6 mmol)
respectively at room temperature under nitrogen atmosphere with stirring. The
reaction
mixture was heated at reflux for 1.5 h during which time a white solid
precipitated out. The
reaction mixture was cooled to room temperature and diluted with 150 mL of
ethyl acetate.
The organic layer was washed with 1N HCI, water, brine, and dried over MgS04.
Upon
25 concentration, a yellow syrup (1.8 g) was obtained. The crude product was
purified by flash
chromatography on silica gel with ethyl acetate/hexanes 1:9 as eluent to
provide 1.22 g of
the title compound, a compound of the invention, as a white solid melting at
65-66 °C.
1H NMR: (300 MHz, CDCl3) 8 7.22 (m, 2H), 7.11 (m, 2H), 5.78 (m, 1H), 5.26 (m,
2H), 4.42 (m, 1H), 4.07 (d, 2H), 1.20 (d, 6H).
30 EXAMPLE 4
Step A: Preparation of phenylhvdroxycarbamate
To a stirred solution of NaHC03 (60.5 g) in water (200 mL) in a 2 L beaker was
added portion-wise over 15 min 27.5 g of hydroxylamine hydrochloride. Once the
bubbling
subsided, dichloromethane (200 mL) was added to the reaction mixture and
cooled to S °C.
35 Phenyl chloroformate (50 g) was then added at a steady rate to the reaction
mixture. The
reaction mixture was allowed to warm to room temperature and stirred for 1 h.
Ethyl acetate
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(100 mL) was employed to bring the reaction mixture to a transparent solution.
The organic
layer was separated, washed with brine (200 mL) and dried over MgS04. The
organic
solvent was removed under reduced pressure to give the title compound (38.20
g) as a white
solid melting at 104-107 °C.
Sten B: Preparation of N hvdroxv-2.2-dimethylhvdrazinecarboxamide
To a solution of 37.3 g of the compound of Step A in tetrahydrofuran (200 mL)
at
room temperature under nitrogen was added 22 mL of 1,1-dimethylhydrazine. The
reaction
mixture was then heated at reflux overnight. The solvent was removed under
reduced
pressure to afford an oil which was purified by column chromatography with 9:1
ethyl
acetate-methanol as eluent to give a semi-solid. Triturating of the residue
with
dichloromethane gave the title compound (7.25 g) as a white solid melting at
115-118 °C.
1 H NMR (DMSO-d6) 8 8.5 (brs, 1 H), 8.27 (brs, 1 H), 7.4 (brs, 1 H), 2.4 (s,
6H).
Step C: Preparation of 4-(dimethylamino)-1 2 4-oxadiazolinedine-3 5-dione
The compound of Step B (4.25 g, 29 mmol) was suspended in tetrahydrofuran
(25 mL) at S °C under nitrogen. To the mixture was added portion-wise
1,1'-
carbonyldiimidazole (5.78 g, 29 mmol) while maintaining the reaction
temperature under
10 °C. The reaction was partitioned between ethyl acetate (125 mL) and
1N HCl (60 mL).
The organic layer was separated. The aqueous layer was further extracted with
ethyl acetate
(2 x 100 mL). The combined organic layers were dried over MgS04 and
concentrated under
reduced pressure to afford the title compound as an oil (2.9 g).
1H NMR (CDC13) 8 5.1 (br s, 1H), 2.9 (s, 6H).
Step D: Preparation of 4-(dimethylamino)-N (4-fluorophenyl)-N (1-methylethyl)-
3,5-dioxo-1,2,4-oxadiazolidine-2-carboxamide
The compound of Step D, Example 1 (1.48 g, 6.9 mmol), 4-dimethylaminopyridine
(0.84 g, 6.9 mmol), and the compound of Step C (1.00 g, 6.9 mmol) were
combined in
toluene (25 mL) at room temperature. The reaction mixture was heated to 80
°C for 3 h.
Acetonitrile (20 mL) and silica gel (5 g) were added and the solvent was
removed under
reduced pressure. After column chromatography with 8:2 hexanes-ethyl acetate
as eluent,
the title compound, a compound of the invention, was isolated as a white solid
( 1.23 g)
melting at 69-71 °C.
iH NMR (CDC13) 8 7.2 (m, 2H), 7.1 (m, 2H), 4.6 (m, 1H), 2.9 (s, 6H), 1.2 (d,
6H).
EXAMPLE 5
Step A: Preparation of 4-f(2-meth lY phenyl)methyl]-3-(phenylmethoxv)-1 2 4-
oxadiazol-5(4I~-one
A SO mL round bottom flask equipped with a thermometer, a stirrer, and a
nitrogen
inlet was charged with 3-(phenylmethoxy)-1,2,4-oxadiazol-5(4H)-one (Synthesis,
(1991),
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265 0.5 g, 2.6 mmol), potassium carbonate (0.5 g, 3.6 mmol),
tetrabutylammonium bromide
(0.022 g, 0.1 mmol), 2-methylbenzyl bromide (0.6 g, 3.2 mmol) and acetonitrile
(10 mL).
The reaction mixture was stirred at room temperature for 18 h. The reaction
mixture was
poured into water (25 mL) and extracted with dichloromethane (3 x 20 mL),
dried over
MgS04 and concentrated under reduced pressure to provide a solid. The solid
was further
purified by flash chromatography on silica gel using 9:1 hexane-ethyl acetate
to provide 0.3
g (40%) of the title compound as a white solid melting at 77-78 °C.
1H NMR (CDC13): 8 7.39 (m, 3H), 7.27 (m, 3H), 7.17 (m, 3H), 5.26 (s, 2H), 4.69
(s, 2H), 2.31 (s, 3H).
Step B: Preparation of N (4-chlorophenyl)-N ( 1-methvleth~l-4-j(2-
methylphenyl)methyll-3.5-dioxo-1,2,4-oxadiazolidine-2-carboxamide
A 50 mL round bottom flask equipped with a stirrer, a thermometer, and a
nitrogen
inlet was charged with the compound of Step A (0.6 g, 2.05 mmol), (4-
chlorophenyl)(1-
methylethyl)carbamic chloride (0.5 g, 2.155 mmol), N, N'-dimethylaminopyridine
(0.26 g,
2.13 mmol) and tetrahydrofuran (20 mL). The mixture was heated to reflux for 3
hours, then
cooled to room temperature and poured into 1N HCl (50 mL). The mixture was
extracted
with diethyl ether (3 x 25 mL). The organic layer was dried over MgS04 and
concentrated
under reduced pressure to provide a thick oil. The oil was purified by flash
chromatography
on silica gel using 9:1 hexane-ethyl acetate to provide 0.22 g (28%) of the
title compound as
a white solid melting at 90-91 °C.
1H NMR (CDCl3): 8 7.5-7.0 (m, 8H), 4.63 (s, 2H), 4.6 (m, 1H), 2.36 (s, 3H),
1.18
(d, 6H).
EXAMPLE 6
Step A: Preparation of 4-methyl-3-(phenylmethoxy)-1 2 4-oxadiazol-5~4 -one
A 50 mL round bottom flask equipped with a thermometer, a stirrer and a
nitrogen
inlet was charged with 3-(phenylinethoxy)-1,2,4-oxadiazol-5(4H)-one (1 g, 5.2
mmol),
iodomethane (0.916 g, 6.5 mmol), 1,8-diazabicyclo[5.4.0]undec-7-ene (1 g, 6.5
mmol) and
acetonitrile (10 mL). The mixture was stirred at room temperature for 18 h.
The entire
reaction mixture was flash chromatographed (silica gel, 8:2 hexane-ethyl
acetate) to provide
1 g (37.5%) of the title compound as a white solid melting at 80-83 °C.
1H NMR (CDCIg): 8 7.43 (m, SH), 5.32 (s, 2H), 3.09 (s, 3H).
S, tep B: Preparation ofN (4-fluorophen"~I,)-4-methyl-N (1-methyleth,~l)-3,5-
dioxo-
1,2,4-oxadiazolidine-2-carboxamide
A 50 mL round bottom flask equipped with a thermometer, a stirrer and a
nitrogen inlet
was charged with 4-methyl-3-(phenylmethoxy)-1,2,4-oxadiazol-5(4F~-one (0.55 g,
2.66
mmol), (4-fluorophenyl)(1-methylethyl)carbamic chloride (0.581 g, 2.7 mmol),
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43
N, N'-dimethylaminopyridine (0.329 g, 2.7 mmol) and acetonitrile (10 mL). The
reaction
mixture was heated to reflux 2 h, and allowed to cool to room temperature. The
entire mixture
was flash chromatographed (silica gel, 9:1, then 8:2 hexane-ethyl acetate) to
provide 0.6 g
(76%) of the title compound as a white solid melting at 135-136 °C.
1H NMR (CDCl3) 8 7.29 (m, 2H), 7.11 (m, 2H), 4.64 (m, 1H), 3.05 (s, 3H), 1.18
(d,
6H).
EXAMPLE 7
St-ep A: Preparation of N (4-chlorophenvl)-4-methyl-N ( 1-methvlethyl)-3 5-
dioxo-
1.2.4-oxadiazolidine-2-carboxamide
A 50 mL round bottom flask, equipped with a thermometer, a stirrer and
nitrogen
inlet was charged with 3-(phenylmethoxy)-1,2,4-oxadiazol-S(4H)-one (0.5 g, 2.6
mmol),
1,8-diazabicyclo[5.4.0]unded-7-ene (0.5 g, 3.28 mmol), iodomethane (0.5 g,
3.54 mmol) and
acetonitrile (5 mL). The mixture was stirred at room temperature for 18 h. To
the mixture
was added (4-chlorophenyl)( 1-methylethyl)carbamic chloride (0.7 g, 3 mmol)
and N,
N'-dimethylamino-pyridine (0.367 g, 3 mmol), and the resulting mixture was
heated to
reflex for 2 h. It was then cooled to room temperature and flash
chromatographed (silica gel,
9:1 hexane-ethyl acetate) to provide 150 mg (18 %) of the title compound as a
white solid
melting at 121-123 °C.
1H NMR (CDCl3): 8 7.36 (m, 2H), 7.2 (m, 2H), 4.6 (m, 1H), 3.05 (s, 3H), 1.21
(d,
6H).
EXAMPLE 8
Step A: Preparation of 4-(2-methylpropyl)-3-(nhenylmethoxy)-1 2 4-oxadiazol-
5(4F~-
one
A 50 mL round bottom flask equipped with a thermometer, a stirrer, addition
funnel
and nitrogen inlet was charged with 3-(phenylmethoxy)-1,2,4-oxadiazol-5(4H)-
one (1 g, 5.2
mmol), 2-methyl propanol (0.45 g, 6 mmol), triphenylphosphine (1.57 g, 6 mmol)
and
tetrahydrofuran (5 mL). The mixture was cooled to 0 °C and a solution
of diethyl
azodicarboxylate (1.04 g, 6 mmol) in tetrahydrofuran (2 mL) was added dropwise
over a
period of 10 min. The reaction mixture was allowed to warm to room
temperature, and
stirred for 18 h. The entire mixture was flash chromatographed (silica gel,
8:2 hexane-ethyl
acetate) to provide 1.1 g (84 %) of the title compound as a white solid
melting at 53-60 °C.
1H NMR (CDCl3): 8 7.42 (m, SH), 5.31 (s, 2H), 3.34 (d, 2H), 2.01 (m, 1H),
0.897 (d,
6H).
Step B: Preparation of N (4-fluorophenyl)-N (1-methylethyl)-4-(2-meth~nrop~)-
3,5-
dioxo-1.2.4-oxadiazolidine-2-carboxamide
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A 50 mL round bottom flask equipped with a stirrer, a thermometer and a
nitrogen
inlet was charged with 4-(2-methylpropyl)-3-(phenylmethoxy)-1,2,4-oxadiazol-
S(4I~-one
(0.25 g, 1 mmol), (4-fluorophenyl)(1-methylethyl)carbamic chloride (0.24 g,
1.1 mmol),
N, N'-dimethylaminopyridine (0.14 g, 1.1 mmol) and acetonitrile (10 mL). The
mixture was
heated to reflux for 2 h and allowed to cool to room temperature. The entire
mixture was
flashed chromatographed (silica gel, 9:1 hexane-ethyl acetate) to provide 0.18
(53 %) of the
title compound as a white solid melting at 80-81 °C.
1H NMR (CDC13): 8 7.24 (m, 2H), 7.11 (m, 2H), 4.65 (m, 1H), 3.29 (d, 2H), 2.0
(m,
1 H), 1.2 (d, 6H), 0.89 (d, 6H).
EXAMPLE 9
Step A: Preparation ofN (4-fluorophen~)-N (1-methylethyl)-3 5-dioxo-4
(phenylmethyl)-1,2.4-oxadiazolidine-2-carboxamide
A 50 mL round bottom flask equipped with a thermometer, a stirrer and a
nitrogen
inlet was charged with 3-(phenyhnethoxy)-1,2,4-oxadiazol-5(41-one (0.5 g, 2.6
mmol),
(4-fluorophenyl)(1-methylethyl)carbamic chloride (0.58 g, 27 mmol),
N, N'-dimethylaminopyridine (0.33 g, 2.7 mmol) and acetonitrile (S mL). The
mixture was
heated to reflux for 3 h and allowed to cool to room temperature. The mixture
was flash
chromatographed (silica gel, 9:1 hexane-ethyl acetate) to provide 0.24 g (25
%) of the title
compound as a white solid melting at 95-96 °C.
1H NMR (CDCl3): 8 7.22 (s, SH), 7.2 (m, 2H), 7.06 (m, 2H), 4.6 (m, 1H), 4.59
(s,
2H), 1.17 (d, 6H).
EXAMPLE 10
Step A: Preparation of N (4-fluoronhenyl)-N ( 1-methylethyl)-3,5-dioxo-1,2.4-
oxadiazolidine-2-carboxamide and N (4-fluorophenvl)-4-methyl-N (1-
methvlethvl)-3,5-dioxo-1,2.4-oxadiazolidine-2-carboxamide
A 50 mL round bottom flask equipped with a thermometer, a stirrer and nitrogen
inlet
was charged with 3-methoxy-1,2,4-oxadiazol-S(4ht)-one (1.16 g, 0.01 m), (4-
fluorophenyl)(1-methylethyl)carbamic chloride (2.4 g, 0.011 m),
N, N'-dimethylaminopyridine (1.35 g, 0.011 m) and acetonitrile (20 mL). The
mixture was
heated to reflux for 18 h. The mixture was allowed to cool to room
temperature, poured into
1N HCl (20 mL) and extracted with ethyl acetate (3 x 25 mL). The organic phase
was dried
over MgS04 and concentrated under reduced pressure to provide a thick oil. The
oil was
flash chromatographed (silica gel, 7:3 dichloromethane-ethyl acetate) to
provide two
fractions. Fraction A contained 0.42 g (15%) ofN (4-fluorophenyl)-4-methyl-N
(1-
methylethyl)-3,5-dioxo-1,2,4-oxadiazolidine-2-carboxamide as a white solid
melting at
135-136 °C. 1H NMR (CDC13): 8 7.26 (m, 2H), 7.11 (m, 2H), 4.6 (m, 1H),
3.05 (s, 3H),
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1.17 (m, 6H). Fraction B contained 1.1 g (40 %) of N (4-fluorophenyl)-N (1-
methylethyl)-
3,5-dioxo-1,2,4-oxadiazolidine-2-carboxamide as a solid melting at 55-60
°C.
1H NMR (CDC13): 8 7.24 (m, 2H), 7.19 (m, 2H), 4.6 (m, 1H), 1.2 (d, 6H). IR
(CHZCl2); 3200, 3300, 1776, 1715 cm-1. MS (M + 1): 281, 257.
5 Sten B: Preparation ofN (4-fluorophenyl~l-methyleth~)-4-(2-meth~nropyl)-3 5-
dioxo-1.2.4-oxadiazolidine-2-carboxamide
A 50 mL round bottom flask equipped with a thermometer, a stirrer, an addition
funnel, and a nitrogen inlet was charged with N (4-fluorophenyl)-N (1-
methylethyl)-3,5-
dioxo-1,2,4-oxadiazolidine-2-carboxamide (5.5 g, 0.019 m), 2-methyl-1-propanol
(3 g, 0.04
10 mol), triphenylphosphine (6.3 g, 0.021 mol) and tetrahydrofuran (60 mL).
The reaction
solution was cooled to 1 S °C and diethyl azodicarboxylate (4.2 g,
0.024 mol) in
tetrahydrofuran (10 mL) was added dropwise over a period of 10 min. The
reaction mixture
was stirred at room temperature for 18 h. The solvent was removed under
reduced pressure
and the residue was flash chromatographed (silica gel, 9:1 hexane-ethyl
acetate) to provide
15 the title compound as a white solid (5.6 g, 88%). The solid has a melting
range of 80-81 °C,
and was identical to the material prepared in Example 8, Step B.
EXAMPLE 11
Step A: Preparation of methyl (chlorocarbonyl,~(2 6-dimethylphenyl)carbamate
A mixture of toluene (150 mL), biphenyl (0.2 g) and sodium methoxide in
methanol
20 (23.76 g, 0.11 mol, 25% by weight) was heated at reflux, and the methanol-
toluene
azeotrope was removed. The mixture was allowed to cool to 80 °C, and
toluene (80 mL)
was added. To the resulting mixture was added in five portions methyl (2,6-
dimethylphenyl)carbamate ( 17.9 g, 0.1 mol). The methanol formed in the
reaction was
removed as the above azeotrope. When most of the methanol had been removed,
ethylene
25 glycol dimethyl ether (8 mL) was added, and the mixture was distilled until
the head
temperature reached 110 °C. The mixture was allowed to cool to 25
°C, and ethylene glycol
dimethyl ether (3 mL) was added. The mixture was then added to phosgene in
toluene (22.5
g, 0.56 mol, 25% by weight). When the addition was complete, excess phosgene
was
removed by distillation. The mixture was allowed to cool to 25 °C, and
then washed with
30 sodium bicarbonate solution (40 mL, saturated). The organic layer was dried
and the
volatiles removed by evaporation to give 17.21 g (64.5%) of the title compound
as a solid.
An analytical sample was prepared by column chromatography on silica gel using
1:3 ethyl
acetate-hexanes as the eluent.
M.P. 84.5-86 °C; IR (Nujol): 1814, 1437, 1252, 1229, 1209, 1182, 1013,
982, 845
35 cm-1; 1H NMR (CDC13): 8 7.28-7.12 (m, 3H), 3.82 (s, 3H), 2.23 (s, 6H).
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Step B: Preparation of 4-(2 6-dimethylphen r~,l -2-methvl-1 2 4-oxadiazolidine-
3 5-
dione
A portion of the compound from Step A (3.72 g, 15.4 mmol) in dioxane ( 15 mL)
was
added to a mixture of aqueous hydroxylamine (2.03 g, 30.7 mmol, 50% by weight)
in
dioxane ( 15 mL). When the addition was complete, a solution of potassium
hydroxide (2.22
g, 33.6 mmol, 85 %) in water (5 mL) was added dropwise to the mixture so that
the
temperature did not rise beyond 30 °C. When the addition was complete,
the solvent was
removed until the volume was reduced to about 5 mL. The mixture was poured
into water
(100 mL), and the aqueous mixture was extracted with ethyl acetate (2 x 50
mL). The
aqueous mixture was acidified with HCl and further extracted with ethyl
acetate (2 x SO mL).
The combined organic extracts from the second extraction were dried and
evaporated to give
the title compound as a solid (2.34 g, 73.7%). The solid has a melting point
range of 92-93.5
°C after crystallization from ether/hexanes, and was identical to
material prepared in
Example 2, Step B.
EXAMPLE 12
Step A: Preparation of N'-hydroxy-N ( 1-methylethyl)-N phenylurea
A solution of SO% aqueous hydroxylamine (16.8 g, 0.25 mol) was added dropwise
to a
solution of (1-methylethyl)phenylcarbamic chloride (20.0 g, 0.1 mol) in 200 mL
of THF in
an ice bath so that the reaction temperature was kept below 30 °C.
Precipitate began to form
halfway through the addition. The resulting slurry was stirred overnight. The
mixture was
filtered, and the solids collected were first washed with water and then with
hexane/ether.
After air-drying, 14.56 g of the title compound was obtained. Its structure
was confirmed by
an analysis of the NMR spectra. The filtrate was stripped down to afford a
residue which
was washed sequentially with 1N HCI, water and hexane/ether to yield a second
crop of the
title compound (5.38 g) melting at 165-166 °C. The combined yield was
100%.
1H NMR (300 MHz, DMSO-d6): 8 8.10 (br s, 1H), 7.74 (s, 1H), 7.38 (m, 3H), 7.12
(m,
2H), 4.55 (m, 1 H), 0.97 (d, 6H)
Step B: Preparation ofN (1-methyleth~)-3 5-dioxo-N phenvl-1 2 4-oxadiazolidine-
2-
carboxamide
A solution of chlorocarbonyl isocyanate (5.0 g, 0.047 mol) was added dropwise
to a
slurry of the title compound of Step A (9.2 g, 0.047 mol) and triethylamine
(5.3 g, 0.052
mol) in 200 mL of THF while maintaining the reaction temperature below 30
°C using an ice
bath. After 2 hours, TLC showed the presence of starting material. Another 0.5
g of
chlorocarbonyl isocyanate was added, and the reaction mixture was stirred for
another hour.
At that point, TLC showed still the presence of starting material. The
reaction mixture was
filtered to remove solids, and the filtrate was stripped to dryness and then
extracted with 1N
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HC1 and ether. Upon evaporation of volatiles, a gummy product was obtained
which was
taken into methylene chloride and potassium carbonate solution. Solids were
collected by a
filtration, washed with methylene chloride and air dried. The solids (5.3 g)
were found to be
the potassium salt of the title compound. The basic aqueous filtrate was
acidified with
concentrated HCl and extracted with methylene chloride to afford 4 g of the
title compound,
an intermediate useful for the preparation of the compounds of the present
invention, melting
at 116-7 °C. From the methylene chloride used to wash the solids, 2.6 g
of the title
compound of Step A was recovered. This represented a 71.7% conversion. The
combined
yield was therefore 96% based on the 71.7% conversion.
1H NMR (300 MHz, DMSO-d6): 8 9.60 (brs, 1H), 7.37 (m, 3H), 7.23 (m, 2H), 4.60
(m, 1 H), 1.19 (d, 6H).
EXAMPLE 13
Step A: Preparation ofN (4-fluorophenyl)-N (1-methylethyl)-3 5-dioxo-1 2 4-
oxadiazolidine-2-carboxamide
A 1 L three neck round bottom flask equipped with nitrogen inlet, thermometer
and
water condenser was charged with dioxanes (400 mL), 1,2,4-oxadiazole-3,5-dione
(30 g 0.29
moles, prepared according to Srivastava, P. and Robins, R., J. Med. Chem.
1981, 24, 1172-
1177), 4-dimethylaminopyridine (36 g, 0.29 mole), and N-isopropyl-4-
flourophenylcarbamoyl chloride (63 g, 0.29 moles) at room temperature. The
yellow
mixture was heated at reflux for 4 hours. When no starting material was
detected by thin
layer chromatography, heat was tuned off and mixture was cooled to room
temperature. The
solvent was removed under reduced pressure and the resulting solids were
suspended in
ethyl acetate. The mixture was washed with 1N HCI, and the aqueous layer was
extracted
twice with ethyl acetate. The combined organic solutions were washed with
brine, dried
over anhydrous magnesium sulfate, and concentrated under reduced pressure. The
product
was crystallized from chlorobutane and hexanes, and filtered to give 47 g
(57%) of the title
compound as a white solid melting at 94-95 °C.
IH NMR: (300 MHz, CDC13) 8 7.24 (m, 2H), 7.09 (m, 2H), 4.63 (m, 1H), 1.18 (d,
6H).
Step B: Preaaration ofN (4-fluorophengirl)-N,4-bis(1-methyleth~)-3,5-dioxo-
1,2,4-
oxadiazolidine-2-carboxamide
A solution of the compound of Step A ( 1.0 g , 3.6 mmol) in 20 mL of
triisopropylorthoformate was heated at 145 °C for 2 h and then allowed
to stir at ambient
temperature overnight. The volatiles were removed under reduced pressure, and
the residue
recrystallized from methanol to give 0.99 g (86%) of the title compound, a
compound of this
invention, as a solid melting at 78-80 °C.
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iH NMR (300 MHz, CDC13): 8 7.26(m, 2H), 7.11(m, 2H), 4.62(m, 1H), 4.18(m, 1H),
1.40(d, 6H), 1.20(d, 6H).
EXAMPLE 14
Step A: Preparation of 2.2'-carbonylbis[~1-methyleth~)-1 2 4-oxadiazolidine-3
S-
dione
To a solution of 4-(1-methylethyl)-1,2,4-oxadiazolidine-3,5-dione (20 g, 139
mmol)
and hexamethylguanidinium chloride (0.25 g, 1.39 mmol) in 150 mL of toluene
was added
phosgene (6.88 g, 69 mmol, 20% by weight in toluene). The resulting mixture
was heated at
reflux for 1.5 h with the use of a dry ice/acetone condenser. The volatiles
were removed
under reduced pressure, and the residue recrystallized from 150 mL of n-BuCI
to give 14 g
(64%) of the title compound as a white solid melting at 150 °C.
1H NMR (300 MHz, CDCl3): 81.52 (d, 6H), 4.36 (m, 1H).
Step B: Preparation ofN.4-bis(1-methylethyl)-3 5-dioxo-N phenyl-1 2 4-
oxadiazolidine-2-carboxamide
A solution of the compound of Step A (0.5 g, 1.6 mmol), N phenyl-N (2-
methylethyl)amine (0.215 g, 1.6 mmol) and 4- dimethylaminopyridine (0.19 g,
1.6 mmol) in
10 mL of acetonitrile was heated at reflux under a nitrogen atmosphere. The
resulting
mixture was allowed to cool to ambient temperature and poured into 25 mL of
water. It was
then extracted with ethylacetate (4 x 25 mL). Condensation gave an oil which
was purified
by flash chromatography using 1:3 EtOAc-Hexanes as the eluant to give the
title compound,
a compound of this invention, as a white solid melting at 83-84 °C.
1H NMR (300 MHz, CDCl3): 8 1.20 (d, 6H), 1.38 (d, 6H), 4.16 (m, 1H), 4.63 (m,
1H),
7.26 (m, 2H), 7.39 (m, 3H).
EXAMPLE 15
Step A: N (4-fluorophenyl)-4-(methoxymethyl~-N (1-methylethyl)-3 S-dioxo-1 2 4-
oxadiazolidine-2-carboxamide
To a solution of 308 uL of bromomethyl methyl ether (1 eq, 90% tech.) in 8 mL
dry
acetonitrile was added 995 mg of the title compound of Step A in Example 13.
To this
mixture was then addede 508 uL (1 eq) of 1,8-diazabicyclo[5.4.0]undec-7-ene
(DBU). The
resulting solution was heated at reflux under a nitrogen atomsphere for 3 h.
The reaction
mixture was allowed to cool to room temperature and the volatiles removed
under reduced
pressure. The residue was dissolved in 1 mL of dichloromethane and loaded onto
a 70 mL
solid phase extraction (SPE) carkridge containing 10 g of silica gel (230-400
mesh). The title
compound (260 mg), a compound of this invention, was obtained after elution
using a 20%
ethyl acetate/hexane solution.
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IH NMR (300 MHz, CDC13): 8 7.22(m, 2H),7.09 (m, 2H), 4.89 (s, 2H), 4.65 (m,
1H),
3.39 (s, 3H), 1.2 (d, 6H).
By the procedures described herein together with methods known in the art, the
following compounds of Tables 1 to 3 can be prepared. The following notations
have been
used in Tables.
Q-1 Ph Q-36 2-SCH3-PhPh
Q-2 2-Cl-Ph Q-37 2-Me-6-(i-Pr)-Ph
Q-3 3-CI-Ph Q-38 2-Cl-4-Me-Ph
Q-4 4-Cl-Ph Q-39 2-CN-Ph
Q-5 2-Br-Ph Q-40 4-Cl-2-Me-Ph
Q-6 2-F-Ph Q-41 2-CI-6-Me-Ph
Q-76 2,4-di-F-Ph Q-42 2-Me-5-Cl-Ph
Q-8 2,6-di-F-Ph Q-43 2-Cl-S-Me-Ph
Q-9 2,3-di-CI-Ph Q-44 2-Cl-3-Me-Ph
Q-10 2,4-di-Cl-Ph Q-45 2-NO -Ph
Q-11 2,6-di-CI-Ph Q-46 1-tetrahydronaphthyl
Q-12 2,6-di-Et-Ph Q-47 4-(2,3-dihydro-1H-indene)
Q-13 2,6-di-OMe Q-48 7-(2,3-diH-2,2-di-Me-7-benzofuran)
Q-14 2-Cl-4-F-Ph Q-49 2-Vinyl-Ph
Q-15 2-Cl-6-F-Ph Q-50 2-Ph-Ph
Q-16 2-Me-Ph Q-51 1-(2-Me-tetrahydronaphthyl)
Q-17 3-Me-Ph Q-52 3-(2-CI-Pyridine)
Q-18 4-Me-Ph Q-53 4,6-di-Me P
- yrimidin-5-yl
Q-19 2-Et-Ph Q-54 4,6-di-OMe P
- yrimidin-5-yl
Q-20 2-Pr-Ph Q-55 PhCH -
Q-21 2,5-di-Me-Ph Q-56 PhC(CH )-
Q-22 4-OMe-Ph Q-57 (2-CI-Ph)CH
Q-23 2-Cl-6-Me-Ph Q-58
(2,6-di-Cl-Ph)CH -
Q-24 2,6-di-Me-Ph Q-59
(2,3-di-CI-Ph)CH -
Q-25 2,4-di-Me-Ph Q-60 (2-Me-Ph)CH -
Q-26 2,5-di-Me-Ph Q-61
(2-OCH -Ph)CH -
Q-27 2,3-di-Me-Ph Q-62
(2,4-di-Cl-Ph)CH -
Q-28 2-Me-6-Et-Ph Q-63 (2-CF -Ph)CH -
Q-29 2-CF -Ph Q-64 (2-OCF -Ph)CH -
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Q-30 4-CF -Ph Q-65
(2-CN-Ph)CH2-
Q-31 2-OCF H-Ph Q-66 (2-Cl-Ph)CH(CH )-
Q-32 2-OCF -Ph Q-67 (2-Me-Ph)CH(CH )-
Q-33 2,4,6-tri-Me-PhQ-68 PhCH CH -
Q-34 4-Cl-2,6-di-Me-PhQ-69
(2-Cl-Ph)CH CH -
Q-35 2-OPh-Ph Q-70 (2-Me-Ph)CH CH -
H3 H3 H3
CH3 ~ ~ C2H5 ~ ~ ~ ~ CH3
O O O O
Q-71 Q-72 Q-73 Q-74
~3 H3 H3 H3 Cl
CH3
O S S S
Q-75 Q-76 Q-77 Q-78
CH3 H3 CH3 H3
H3 S ~ ~3 ~ ~ ~ Cl
Q-79 ~3
Q-80 ~3 ~3
Q-81 Q-82
H3
S S
~3 Q-84 Q-85 Q-86
Q-83
~3 H3
S
Q-88 H3 O
Q-87 Q-89 Q-90
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H3
S' ~'° ~~
Q-91 Q-~ S
Q-93 Q-94
Q-95 n-Pr Q-121 c-Butyl
Q-96 n-Bu Q-122 EtC(Me) -
Q-97 i-Bu Q-123 CF CH -
Q-98 n-hex Q-124 4-( 1-Butenyl)
Q-99 c-Pr Q-125 3-Me-Propargyl
Q-100 A11y1 Q-126 1-(3-Me-1-Propenyl)
Q-101 Propargyl Q-127 NCCH -
Q-102 3-(2-Cl-Propenyl)Q-128 (i-C H )O-
Q-103 Cyclohexyl Q-129 (Allyl)O-
Q-104 1-cyclohexenylQ-130 (Me) N
Q-105 2-Me-1-cyclohexenylQ-131 1-piperidino
Q-106 MeOCH CH - Q-132 Me0 S-
Q-107 MeOCH - Q-133 MeSCH CH -
Q-108 3-Cl-Pr Q-134 Me NS(O) -
Q-109 4-( 1,1-di-F-butenyl)Q-135 O NCH -
Q-110 3-(1,1-di-Cl-propenyl)Q-136 MeC(~)-
Q-111 i-Pr Q-137 (i-Pr)OC(=O)-
Q-112 2-OMe-Ph Q-138 EtOC(~)-
Q-113 2-Me-6-OMe-Ph Q-139 Me NC(=O)-
Q-114 2-Cl-Et Q-140 EtOC(=O)CH -
Q-115 3-(2-Me-Propenyl)Q-141 (Me0) P(=O)CH
-
Q-116 t-Bu Q-142 Me NC(=O)CH -
Q-117 MeC(=NOMe)CH Q-143 2-(Tetrahydropyranyl)
-
Q-118 2-Me-(c-Hex) Q-144 (Oxirane)-CH
-
Q-119 Et
Q-120 c-Pentyl
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~N ~ ~ H3C
Q-145 Q-146 O~ H3C Q-148
Q-147
O
\ ( \
\ /
Q-150
Q-149
Q-151 Q-152
O ~ \ CF3
F3C ~N' O H3C ~ O ~ -.
1~Y / N /
Q-153 Q-154
Q-155
Q-156
Q-157 Me NCH CH - Q-167 2-(SF )-Ph
Q-158 Me NCH - Q-168 1-(Morpholino)
Q-159 Me SiCH - Q-169 EtCH(Me)-
Q-160 Me NC(=S)- Q-170 Me CCH
Q-161 3-oxetanyl Q-171 (Et) N-
Q-162 NCCH CH Q-172 MeS-
Q-163 MeOC(=O)CH(CH Q-173 MeSC(=S)-
)-
Q-164 MeOC(=O)CH(i-Pr)-Q-174 4-(2-Butynyl)
Q-165 MeNH Q-175 F CS-
Q-166 2-(NMe )-Ph
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\ \
o o
B-1 B-2 B-3 B-4
~3
/~cH3 \
B-6
B-5 B-7 B-8
i-C3Hi C2H5
O B-11
B-12
B-9 B-10
N ~ N
O
B-13 B-14 B-15 B-16
Allyl Propargyl
B-17 B-18
TABLE 1
O O R13
O R2
O
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R2 is i-C~H~, R13 is 4-F
Q Q Q Q Q Q Q Q Q
Q'1 Q-2 Q-3 Q-4 Q_5 Q_6 Q_7 Q_8 Q_9
Q-10 Q-11 Q-12 Q-13 Q-14 Q-15 Q-16 Q-17 Q-18
Q-19 Q-20 Q-21 Q-22 Q-23 Q-24 Q-25 Q-26 Q-27
Q-28 Q-29 Q-30 Q-31 Q-32 Q-33 Q-34 Q-35 Q-36
Q-37 Q-38 Q-39 Q-40 Q-41 Q-42 Q-43 Q-44 Q-45
Q-46 Q-47 Q-48 Q-49 Q-SO Q-S Q-52 Q-53 Q-54
1
Q-55 Q-56 Q-57 Q-58 Q-59 Q-60 Q-61 Q-62 Q-63
Q-64 Q-65 Q-66 Q-67 Q-68 Q-69 Q-70 Q-71 Q-72
Q-73 Q-74 Q-75 Q-76 Q-77 Q-78 Q-79 Q-80 Q-81
Q-82 Q-83 Q-84 Q-85 Q-86 Q-87 Q-88 Q-89 Q-90
Q-91 Q-92 Q-93 Q-94 Q-95 Q-96 Q-97 Q-98 Q-99
Q-100 Q-101 Q-102 Q-103 Q-104 Q-105 Q-106 Q-107 Q-108
Q-109 Q-110 Q-111 Q-112 Q-113 Q-114 Q-115 Q-116 Q-117
Q-118 Q-119 Q-120 Q-121 Q-122 Q-123 Q-124 Q-125 Q-126
Q-127 Q-128 Q-129 Q-130 Q-131 Q-132 Q-133 Q-134 Q-135
Q-136 Q-137 Q-138 Q-139 Q-140 Q-141 Q-142 Q-143 Q-144
Q-145 Q-146 Q-147 Q-148 Q-149 Q-150 Q-151 Q-152 Q-153
Q-154 Q-155 Q-156 Q-157 Q-158 Q-159 Q-160 Q-161 Q-162
Q-163 Q-164 Q-165 Q-166 Q-167 Q-168 Q-169 Q-170 Q-171
Q-172 Q-173 Q-174 Q-175
R2 is i-C~H~, R13 is 2,4-di-F
Q Q Q Q Q Q Q Q Q
Q-1 Q-2 Q-3 Q-4 Q_5 Q_6 Q_7 Q-8 Q_9
Q-10 Q-11 Q-12 Q-13 Q-14 Q-15 Q-16 Q-17 Q-18
Q-19 Q-20 Q-21 Q-22 Q-23 Q-24 Q-25 Q-26 Q-27
Q-28 Q-29 Q-30 Q-31 Q-32 Q-33 Q-34 Q-35 Q-36
Q-37 Q-38 Q-39 Q-40 Q-41 Q-42 Q-43 Q-44 Q-45
Q-46 Q-47 Q-48 Q-49 Q-50 Q-51 Q-52 Q-53 Q-54
Q-SS Q-56 Q-57 Q-58 Q-59 Q-60 Q-61 Q-62 Q-63
Q-64 Q-65 Q-66 Q-67 Q-68 Q-69 Q-70 Q-71 Q-72
Q-73 Q-74 Q-75 Q-76 Q-77 Q-78 Q-79 Q-80 Q-81
Q-82 Q-83 Q-84 Q-85 Q-86 Q-87 Q-88 Q-89 Q-90
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Q-91 Q-92 Q-93 Q-94 Q-95 Q-96
Q-97 Q-98 Q-99
Q-100 Q-101 Q-102 Q-103 Q-104 Q-105 Q-106
Q-107 Q-108
Q-109 Q-110 Q-111 Q-112 Q-113 Q-114 Q-115 Q-116 Q-117
Q-118 Q-119 Q-120 Q-121 Q-122 Q-123 Q-124 Q-125 Q-126
Q-127 Q-128 Q-129 Q-130 Q-131 Q-132 Q-133 Q-134 Q-135
Q-136 Q-137 Q-138 Q-139 Q-140 Q-141 Q-142 Q-143 Q-144
Q-145 Q-146 Q-147 Q-148 Q-149 Q-150 Q-151 Q-152 Q-153
Q-154 Q-155 Q-156 Q-157 Q-158 Q-159 Q-160 Q-161 Q-162
Q-163 Q-164 Q-165 Q-166 Q-167 Q-168 Q-169 Q-170 Q-171
Q-172 Q-173 Q-174 Q-175
R2 is i-C~H7, R13 is 4-CI
Q Q Q Q Q Q Q Q Q
Q-I Q-2 Q-3 Q-4 Q_5 Q_6 Q_7 Q_8 Q_9
Q-10 Q-11 Q-12 Q-13 Q-14 Q-15 Q-16 Q-17 Q-18
Q-19 Q-20 Q-21 Q-22 Q-23 Q-24 Q-25 Q-26 Q-27
Q-28 Q-29 Q-30 Q-31 Q-32 Q-33 Q-34 Q-35 Q-36
Q-37 Q-38 Q-39 Q-40 Q-41 Q-42 Q-43 Q-44 Q-45
Q-46 Q-47 Q-48 Q-49 Q-50 Q-51 Q-52 Q-53 Q-54
Q-55 Q-56 Q-57 Q-58 Q-59 Q-60 Q-61 Q-62 Q-63
Q-64 Q-65 Q-66 Q-67 Q-68 Q-69 Q-70 Q-71 Q-72
Q-73 Q-74 Q-75 Q-76 Q-77 Q-78 Q-79 Q-80 Q-81
Q-82 Q-83 Q-84 Q-85 Q-86 Q-87 Q-88 Q-89 Q-90
Q-91 Q-92 Q-93 Q-94 Q-95 Q-96 Q-97 Q-98 Q-99
Q-100 Q-101 Q-102 Q-103 Q-104 Q-105 Q-106 Q-107 Q-108
Q-109 Q-110 Q-111 Q-112 Q-113 Q-114 Q-115 Q-116 Q-117
Q-118 Q-119 Q-120 Q-121 Q-122 Q-123 Q-124 Q-125 Q-126
Q-127 Q-128 Q-129 Q-130 Q-131 Q-132 Q-133 Q-134 Q-135
Q-136 Q-137 Q-138 Q-139 Q-140 Q-141 Q-142 Q-143 Q-144
Q-145 Q-146 Q-147 Q-148 Q-149 Q-150
Q-151 Q-152 Q-153
Q-154 Q-155 Q-156 Q-157 Q-158 Q-159 Q-160 Q-161 Q-162
Q-163 Q-164 Q-165 Q-166 Q-167 Q-168 Q-169 Q-170 Q-171
Q-172 Q-173 Q-174 Q-175
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R2 is i-C~H~, R13 is H
Q Q Q Q Q Q Q Q Q
Q-1 Q-2 Q-3 Q-4 Q-5 Q_6 Q_7 Q_8 Q_9
Q-10 Q-11 Q-12 Q-13 Q-14 Q-15 Q-16 Q-17 Q-18
Q-19 Q-20 Q-21 Q-22 Q-23 Q-24 Q-25 Q-26 Q-27
Q-28 Q-29 Q-30 Q-31 Q-32 Q-33 Q-34 Q-35 Q-36
Q-37 Q-38 Q-39 Q-40 Q-41 Q-42 Q-43 Q-44 Q-45
Q-46 Q-47 Q-48 Q-49 Q-50 Q-51 Q-52 Q-53 Q-54
Q-55 Q-56 Q-57 Q-58 Q-59 Q-60 Q-61 Q-62 Q-63
Q-64 Q-65 Q-66 Q-67 Q-68 Q-69 Q-70 Q-71 Q-72
Q-73 Q-74 Q-75 Q-76 Q-77 Q-78 Q-79 Q-80 Q-81
Q-82 Q-83 Q-84 Q-85 Q-86 Q-87 Q-88 Q-89 Q-90
Q-91 Q-92 Q-93 Q-94 Q-95 Q-96 Q-97 Q-98 Q-99
Q-100 Q-101 Q-102 Q-103 Q-104 Q-105 Q-106 Q-107 Q-108
Q-109 Q-110 Q-111 Q-112 Q-113 Q-114 Q-115 Q-116 Q-117
Q-118 Q-119 Q-120 Q-121 Q-122 Q-123 Q-124 Q-125 Q-126
Q-127 Q-128 Q-129 Q-130 Q-131 Q-132 Q-133 Q-134 Q-135
Q-136 Q-137 Q-138 Q-139 Q-140 Q-141 Q-142
Q-143 Q-144
Q-145 Q-146 Q-147 Q-148 Q-149 Q-150 Q-151 Q-152 Q-153
Q-154 Q-155 Q-156 Q-157 Q-158 Q-159 Q-160 Q-161 Q-162
Q-163 Q-164 Q-165 Q-166 Q-167 Q-168 Q-169 Q-170 Q-171
Q-172 Q-173 Q-174 Q-175
Q R2 R13 Q R2 R13 Q R2 R13
Q-2 CH 4-F Q-2 CH 2,4-di-FQ-2 CH 4-C1
Q-16 CH 4-F Q-16 CH 2,4-di-FQ-16 CH 4-Cl
Q-24 CH 4-F Q-24 CH 2,4-di-FQ-24 CH 4-Cl
Q-29 CH 4-F Q-29 CH 2,4-di-FQ-29 CH 4-Cl
Q-57 CH 4-F Q-57 CH 2,4-di-FQ-57 CH 4-Cl
Q-71 CH 4-F Q-71 CH 2,4-di-FQ-71 CH 4-Cl
Q-100 CH 4-F Q-100 CH 2,4-di-FQ-100 CH 4-Cl
Q-119 CH 4-F Q-119 CH 2,4-di-FQ-119 CH 4-Cl
Q-120 CH 4-F Q-120 CH 2,4-di-FQ-120 CH 4-Cl
Q-126 CH 4-F Q-126 CH 2,4-di-FQ-126 CH 4-Cl
Q-130 CH 4-F Q-130 CH 2,4-di-FQ-130 CH 4-Cl
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Q-144 CH 4-F Q-144 CH 2,4-di-FQ-144 CH 4-CI
Q-162 CH 4-F Q-162 CH 2,4-di-FQ-162 CH 4-Cl
Q-169 CH 4-F Q-169 CH 2,4-di-FQ-169 CH 4-CI
Q-2 C2H 4-F Q-2 C2H 2,4-di-FQ-2 C H 4-Cl
Q-16 C H 4-F Q-16 C H 2,4-di-FQ-16 C H 4-C1
Q-24 C H 4-F Q-24 C H 2,4-di-FQ-24 C H 4-Cl
Q-29 C H 4-F Q-29 C H 2,4-di-FQ-29 C H 4-Cl
Q-57 C2H 4-F Q-57 C2H 2,4-di-FQ-57 C H 4-CI
Q-71 C H 4-F Q-71 C H 2,4-di-FQ-71 C H 4-CI
Q-100 C H 4-F Q-100 C H 2,4-di-FQ-100 C H 4-CI
Q-119 C H 4-F Q-119 C H 2,4-di-FQ-119 C H 4-C1
Q-120 C2H 4-F Q-120 C2H 2,4-di-FQ-120 C H 4-CI
Q-126 C H 4-F Q-126 C H 2,4-di-FQ-126 C H 4-C1
~Q-130 C H 4-F Q-130 C H 2,4-di-FQ-130 C H 4-CI
Q-144 C H 4-F Q-144 C H 2,4-di-FQ-144 C H 4-C1
Q-162 C2H 4-F Q-162 C H 2,4-di-FQ-162 C H 4-CI
Q-169 C H 4-F Q-169 C H 2,4-di-FQ-169 C H 4-C1
Q-2 i-C H 4-F Q-2 i-C 2,4-di-FQ-2 i-C H 4-Cl
H
Q-16 i-C H 4-F Q-16 i-C 2,4-di-FQ-16 i-C H 4-CI
H
Q-24 i-C4H 4-F Q-24 i-C4H 2,4-di-FQ-24 i-C H 4-Cl
Q-29 i-C H 4-F Q-29 i-C 2,4-di-FQ-29 i-C H 4-CI
H
Q-57 i-C H 4-F Q-57 i-C 2,4-di-FQ-57 i-C H 4-Cl
H
Q-71 i-C H 4-F Q-71 i-C 2,4-di-FQ-71 i-C H 4-Cl
H
Q-100 i-C4H 4-F Q-100 i-C4H 2,4-di-FQ-100 i-C4H 4-CI
Q-119 i-C H 4-F Q-119 i-C 2,4-di-FQ-119 i-C H 4-CI
H
Q-120 i-C H 4-F Q-120 i-C 2,4-di-FQ-120 i-C H 4-Cl
H
Q-126 i-C H 4-F Q-126 i-C 2,4-di-FQ-126 i-C H 4-Cl
H
Q-130 i-C4H9 4-F Q-130 i-C4H 2,4-di-FQ-130 i-C H 4-Cl
Q-144 i-C H 4-F Q-144 i-C 2,4-di-FQ-144 i-C H 4-C1
H
Q-162 i-C H 4-F Q-162 i-C 2,4-di-FQ-162 i-C H 4-CI
H
Q-169 i-C H 4-F Q-169 i-C4H 2,4-di-FQ-169 i-C H 4-Cl
Q-2 n-C H 4-F Q-2 n-C 2,4-di-FQ-2 n-C H 4-CI
H
Q-16 n-C H 4-F Q-16 n-C 2,4-di-FQ-16 n-C H 4-CI
H
Q-24 n-C H 4-F Q-24 n-C 2,4-di-FQ-24 n-C H 4-CI
H
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Q-29 n-C H 4-F Q-29 n-C H 2,4-di-FQ-29 n-C H 4-C1
Q-57 n-C H 4-F Q-57 n-C H 2,4-di-FQ-57 n-C H 4-Cl
Q-71 n-C H 4-F Q-71 n-C H 2,4-di-FQ-71 n-C H 4-C1
Q-100 n-C H 4-F Q-100 n-C H 2,4-di-FQ-100 n-C H 4-C1
Q-119 n-C H 4-F Q-119 n-C H 4-F Q-119 n-C H 4-F
Q-120 n-C H 4-F Q-120 n-C H 4-F Q-120 n-C H 4-F
Q-126 n-C H 4-F Q-126 n-C H 4-F Q-126 n-C H 4-F
Q-130 n-C H 4-F Q-130 n-C H 4-F Q-130 n-C H 4-F
Q-144 n-C H 4-F Q-144 n-C H 4-F Q-144 n-C H 4-F
Q-162 n-C H 4-F Q-162 n-C H 4-F Q-162 n-C H 4-F
Q-169 n-C H 4-F Q-169 n-C H 4-F Q-169 n-C H 4-F
Q-2 Cyclopropyl4-F Q-2 Cyclopropyl2,4-di-FQ-2 Cyclopropyl4-Cl
Q-16 Cyclopropyl4-F Q-16 Cyclopropyl2,4-di-FQ-16 Cyclopropyl4-Cl
Q-24 Cyclopropyl4-F Q-24 Cyclopropyl2,4-di-FQ-24 Cyclopropyl4-CI
Q-29 Cyclopropyl4-F Q-29 Cyclopropyl2,4-di-FQ-29 Cyclopropyl4-CI
Q-57 Cyclopropyl4-F Q-57 Cyclopropyl2,4-di-FQ-57 Cyclopropyl4-Cl
Q-71 Cyclopropyl4-F Q-71 Cyclopropyl2,4-di-FQ-71 Cyclopropyl4-Cl
Q-100 Cyclopropyl4-F Q-100 Cyclopropyl2,4-di-FQ-100 Cyclopropyl4-Cl
Q-119 Cyclopropyl4-F Q-119 Cyclopropyl2,4-di-FQ-119 Cyclopropyl4-Cl
Q-120 Cyclopropyl4-F Q-120 Cyclopropyl2,4-di-FQ-120 Cyclopropyl4-CI
Q-126 Cyclopropyl4-F Q-126 Cyclopropyl2,4-di-FQ-126 Cyclopropyl4-CI
Q-130 Cyclopropyl4-F Q-130 Cyclopropyl2,4-di-FQ-130 Cyclopropyl4-CI
Q-144 Cyclopropyl4-F Q-144 Cyclopropyl2,4-di-FQ-144 Cyclopropyl4-CI
Q-162 Cyclopropyl4-F Q-162 Cyclopropyl2,4-di-FQ-162 Cyclopropyl4-C1
Q-169 Cyclopropyl4-F Q-169 Cyclopropyl2,4-di-FQ-169 Cyclopropyl4-C1
Q R2 R13 Q R2 R13 Q R2 R13
Q-2 i-C 4-OCF Q-2 i-C 4-COOCH Q-2 i-C 3,5-di-F
H H H
Q-16 i-C 4-OCF Q-16 i-C 4-COOCH Q-16 i-C 3,5-di-F
H H H
Q-24 i-C 4-OCF Q-24 i-C 4-COOCH Q-24 i-C 3,5-di-F
H H H
Q-29 i-C 4-OCF Q-29 i-C 4-COOCH Q-29 i-C 3,5-di-F
H H H
Q-57 i-C 4-OCF Q-57 i-C 4-COOCH Q-57 i-C 3,5-di-F
H H H
Q-71 i-C 4-OCF Q-71 i-C 4-COOCH Q-71 i-C 3,5-di-F
H H H
Q-100 i-C 4-OCF Q-100 i-C 4-COOCH Q-100 i-C 3,5-di-F
H H H
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Q-119 i-C 4-OCF Q-119 i-C 4-COOCH Q-119 i-C 3,5-di-F
H H H
Q-120 i-C 4-OCF Q-120 i-C 4-COOCH Q-120 i-C 3,5-di-F
H H H
Q-126 i-C 4-OCF Q-126 i-C 4-COOCH Q-126 i-C 3,5-di-F
H H H
Q-130 i-C 4-OCF Q-130 i-C3H 4-COOCH Q-130 i-C 3,5-di-F
H7 H
Q-144 i-C 4-OCF Q-144 i-C 4-COOCH Q-144 i-C 3,5-di-F
H H H
Q-162 i-C 4-OCF Q-162 i-C 4-COOCH Q-162 i-C 3,5-di-F
H H H
Q-169 i-C 4-OCF Q-169 i-C 4-COOCH Q-169 i-C 3,5-di-F
H H H
Q-2 i-C 4-CF Q-2 i-C 4-CH Q-2 i-C 2,4,6-tri-F
H H H
Q-16 i-C 4-CF Q-16 i-C 4-CH Q-16 i-C 2,4,6-tri-F
H H H
Q-24 i-C 4-CF Q-24 i-C 4-CH Q-24 i-C 2,4,6-tri-F
H H H
Q-29 i-C 4-CF Q-29 i-C 4-CH Q-29 i-C 2,4,6-tri-F
H H H
Q-57 i-C 4-CF Q-57 i-C 4-CH Q-57 i-C 2,4,6-tri-F
H H7 H
Q-71 i-C 4-CF Q-71 i-C 4-CH Q-71 i-C 2,4,6-tri-F
H H H
Q-100 i-C 4-CF Q-100 i-C 4-CH Q-100 i-C 2,4,6-tri-F
H H H
Q-119 i-C 4-CF Q-119 i-C 4-CH Q-119 i-C 2,4,6-tri-F
H H H
Q-120 i-C 4-CF Q-120 i-C 4-CH Q-120 i-C 2,4,6-tri-F
H H H
Q-126 i-C 4-CF Q-126 i-C 4-CH Q-126 i-C 2,4,6-tri-F
H H H
Q-130 i-C 4-CF Q-130 i-C 4-CH Q-130 i-C 2,4,6-tri-F
H H H
Q-144 i-C 4-CF Q-144 i-C 4-CH Q-144 i-C 2,4,6-tri-F
H H H
Q-162 i-C 4-CF Q-162 i-C 4-CH Q-162 i-C 2,4,6-tri-F
H H H
Q-169 i-C 4-CF Q-169 i-C 4-CH Q-169 i-C 2,4,6-tri-F
H H H
Q-2 i-C 4-OCH Q-2 i-C 2,4-di-ClQ-2 i-C 2,5-di-F
H H H
Q-16 i-C 4-OCH Q-16 i-C 2,4-di-ClQ-16 i-C 2,5-di-F
H H H
Q-24 i-C 4-OCH Q-24 i-C 2,4-di-ClQ-24 i-C 2,5-di-F
H H H
Q-29 i-C 4-OCH Q-29 i-C 2,4-di-ClQ-29 i-C 2,5-di-F
H H H
Q-57 i-C 4-OCH Q-57 i-C 2,4-di-ClQ-57 i-C 2,5-di-F
H H H
Q-71 i-C 4-OCH Q-71 i-C 2,4-di-ClQ-71 i-C 2,5-di-F
H H H
Q-100 i-C 4-OCH Q-100 i-C 2,4-di-ClQ-100 i-C 2,5-di-F
H H H
Q-119 i-C 4-OCH Q-119 i-C 2,4-di-ClQ-119 i-C 2,5-di-F
H H H
Q-120 i-C 4-OCH Q-120 i-C 2,4-di-ClQ-120 i-C 2,5-di-F
H H H
Q-126 i-C 4-OCH Q-126 i-C 2,4-di-ClQ-126 i-C 2,5-di-F
H H H
Q-130 i-C 4-OCH Q-130 i-C 2,4-di-ClQ-130 i-C 2,5-di-F
H H H
Q-144 i-C 4-OCH Q-144 i-C 2,4-di-ClQ-144 i-C 2,5-di-F
H H H
Q-162 i-C 4-OCH Q-162 i-C 2,4-di-ClQ-162 i-C 2,5-di-F
H H H
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Q-169 i-C 4-OCH Q-169 i-C 2,4-di-ClQ-169i-C 2,5-di-F
H H H
Q-2 i-C 4-CN Q-2 i-C 2-F, Q-2 i-C 4-OCF
H H 4-Cl H H
Q-16 i-C 4-CN Q-16 i-C 2-F, Q-16 i-C 4-OCF
H H 4-Cl H H
Q-24 i-C 4-CN Q-24 i-C 2-F, Q-24 i-C 4-OCF
H H 4-Cl H H
Q-29 i-C 4-CN Q-29 i-C 2-F, Q-29 i-C 4-OCF
H H 4-Cl H H
Q-57 i-C 4-CN Q-57 i-C 2-F, Q-57 i-C 4-OCF
H H 4-Cl H H
Q-71 i-C 4-CN Q-71 i-C 2-F, Q-71 i-C 4-OCF
H H 4-Cl H H
Q-100 i-C 4-CN Q-100 i-C 2-F, Q-100i-C 4-OCF
H H 4-CI H H
Q-119 i-C 4-CN Q-119 i-C 2-F, Q-119i-C 4-OCF
H H 4-Cl H H
Q-120 i-C 4-CN Q-120 i-C 2-F, Q-120i-C 4-OCF
H H 4-Cl H H
Q-126 i-C 4-CN Q-126 i-C 2-F, Q-126i-C 4-OCF
H H 4-Cl H H
Q-130 i-C 4-CN Q-130 i-C 2-F, Q-130i-C 4-OCF
H H 4-Cl H H
Q-144 i-C 4-CN Q-144 i-C 2-F, Q-144i-C 4-OCF
H H 4-Cl H H
Q-162 i-C 4-CN Q-162 i-C 2-F, Q-162i-C 4-OCF
H H 4-Cl H H
Q-169 i-C 4-CN Q-169 i-C 2-F, Q-169i-C 4-OCF
H H 4-Cl H H
Q-2 i-C 4-N02 Q-2 i-C 3,4-di-FQ-2 i-C 4-SCH
H H H
Q-16 i-C 4-NO Q-16 i-C 3,4-di-FQ-16 i-C 4-SCH
H H H
Q-24 i-C 4-NO Q-24 i-C 3,4-di-FQ-24 i-C 4-SCH
H H H
Q-29 i-C 4-NO Q-29 i-C 3,4-di-FQ-29 i-C 4-SCH
H H H
Q-57 i-C 4-NO Q-57 i-C 3,4-di-FQ-57 i-C 4-SCH
H H H
Q-71 i-C 4-NO Q-71 i-C 3,4-di-FQ-71 i-C 4-SCH
H H H
Q-100 i-C 4-NO Q-100 i-C 3,4-di-FQ-100i-C 4-SCH
H H H
Q-119 i-C 4-NO Q-119 i-C 3,4-di-FQ-119i-C 4-SCH
H H H
Q-120 i-C 4-NO Q-120 i-C 3,4-di-FQ-120i-C 4-SCH
H H H
Q-126 i-C 4-NO Q-126 i-C 3,4-di-FQ-126i-C 4-SCH
H H H
Q-130 i-C 4-NO Q-130 i-C 3,4-di-FQ-130i-C 4-SCH
H H H
Q-144 i-C 4-NO Q-144 i-C 3,4-di-FQ-144i-C 4-SCH
H H H
Q-162 i-C 4-NO Q-162 i-C 3,4-di-FQ-162i-C 4-SCH
H H H
Q-169 i-C 4-NO Q-169 i-C 3,4-di-FQ-169i-C 4-SCH
H H H
Q R2 R13 Q R2 R13 Q R2 R13
Q-2 Allyl 4-F Q-2 Allyl 2,4-di-FQ-2 Allyl 4-Cl
Q-16 Allyl 4-F Q-16 Allyl 2,4-di-FQ-16 Allyl 4-Cl
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Q R2 R13 Q R2 R13 Q R2 R13
Q-24 Allyl 4-F Q-24 Allyl 2,4-di-FQ-24 Allyl 4-Cl
Q-29 Allyl 4-F Q-29 Allyl 2,4-di-FQ-29 Allyl 4-CI
Q-57 Allyl 4-F Q-57 Allyl 2,4-di-FQ-57 Allyl 4-CI
Q-71 Allyl 4-F Q-71 Allyl 2,4-di-FQ-71 Allyl 4-Cl
Q-100 Allyl 4-F Q-100 Allyl 2,4-di-FQ-100 Allyl 4-Cl
Q-119 Allyl 4-F Q-119 Allyl 2,4-di-FQ-119 Allyl 4-Cl
Q-120 Allyl 4-F Q-120 Allyl 2,4-di-FQ-120 Allyl 4-Cl
Q-126 Allyl 4-F Q-126 Allyl 2,4-di-FQ-126 Allyl 4-Cl
Q-130 Allyl 4-F Q-130 Allyl 2,4-di-FQ-130 Allyl 4-CI
Q-144 Allyl 4-F Q-144 Allyl 2,4-di-FQ-144 Allyl 4-Cl
Q-162 Allyl 4-F Q-162 Allyl 2,4-di-FQ-162 Allyl 4-CI
Q-169 Allyl 4-F Q-169 Allyl 2,4-di-FQ-169 Allyl 4-Cl
Q-2 OCH 4-F Q-2 OCH 2,4-di-FQ-2 OCH 4-Cl
Q-16 OCH 4-F Q-16 OCH 2,4-di-FQ-16 OCH 4-Cl
Q-24 OCH 4-F Q-24 OCH 2,4-di-FQ-24 OCH 4-Cl
Q-29 OCH 4-F Q-29 OCH 2,4-di-FQ-29 OCH 4-Cl
Q-57 OCH 4-F Q-57 OCH 2,4-di-FQ-57 OCH 4-Cl
Q-71 OCH 4-F Q-71 OCH 2,4-di-FQ-71 OCH 4-CI
Q-100 OCH 4-F Q-100 OCH 2,4-di-FQ-100 OCH 4-Cl
Q-119 OCH 4-F Q-119 OCH 2,4-di-FQ-119 OCH 4-Cl
Q-120 OCH 4-F Q-120 OCH 2,4-di-FQ-120 OCH 4-CI
Q-126 OCH 4-F Q-126 OCH 2,4-di-FQ-126 OCH 4-Cl
Q-130 OCH 4-F Q-130 OCH 2,4-di-FQ-130 OCH 4-Cl
Q-144 OCH 4-F Q-144 OCH 2,4-di-FQ-144 OCH 4-Cl
Q-162 OCH 4-F Q-162 OCH 2,4-di-FQ-162 OCH 4-CI
Q-169 OCH 4-F Q-169 OCH 2,4-di-FQ-169 OCH 4-Cl
Q-2 N(CH 4-F Q-2 N(CH 2,4-di-FQ-2 N(CH 4-Cl
) ) )
Q-16 N(CH 4-F Q-16 N(CH 2,4-di-FQ-16 N(CH 4-Cl
) ) )
Q-24 N(CH 4-F Q-24 N(CH 2,4-di-FQ-24 N(CH 4-Cl
)2 ) )
Q-29 N(CH 4-F Q-29 N(CH 2,4-di-FQ-29 N(CH 4-Cl
) ) )
Q-57 N(CH 4-F Q-57 N(CH 2,4-di-FQ-57 N(CH 4-Cl
) ) )
Q-71 N(CH 4-F Q-71 N(CH 2,4-di-FQ-71 N(CH 4-Cl
) ) )
Q-100 N(CH 4-F Q-100 N(CH 2,4-di-FQ-100 N(CH 4-Cl
)2 )2 )
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Q R2 R13 Q R2 R13 Q R2 R13
Q-119 N(CH ) 4-F Q-119 N(CH 2,4-di-FQ-119 N(CH 4-Cl
) )
Q-120 N(CH ) 4-F Q-120 N(CH 2,4-di-FQ-120 N(CH 4-C1
) )
Q-126 N(CH ) 4-F Q-126 N(CH 2,4-di-FQ-126 N(CH 4-C1
) )
Q-130 N(CH ) 4-F Q-130 N(CH 2,4-di-FQ-130 N(CH 4-Cl
) )
Q-144 N(CH ) 4-F Q-144 N(CH 2,4-di-FQ-144 N(CH 4-C1
) )2
Q-162 N(CH ) 4-F Q-162 N(CH 2,4-di-FQ-162 N(CH 4-C1
) )
Q-169 N(CH ) 4-F Q-169 N(CH 2,4-di-FQ-169 N(CH 4-CI
) )
Q-2 CH OCH 4-F Q-2 CH OCH 2,4-di-FQ-2 CH OCH 4-CI
Q-16 CH OCH 4-F Q-16 CH OCH 2,4-di-FQ-16 CH OCH 4-Cl
Q-24 CH OCH 4-F Q-24 CH OCH 2,4-di-FQ-24 CH OCH 4-CI
Q-29 CH OCH 4-F Q-29 CH OCH 2,4-di-FQ-29 CH OCH 4-Cl
Q-57 CH OCH 4-F Q-57 CH OCH 2,4-di-FQ-57 CH OCH 4-Cl
Q-71 CH20CH 4-F Q-71 CH OCH 2,4-di-FQ-71 CH20CH 4-Cl
Q-100 CH OCH 4-F Q-100 CH OCH 2,4-di-FQ-100 CH OCH 4-CI
Q-119 CH OCH 4-F Q-119 CH OCH 2,4-di-FQ-119 CH OCH 4-CI
Q-120 CH OCH 4-F Q-120 CH OCH 2,4-di-FQ-120 CH OCH 4-CI
Q-126 CH20CH 4-F Q-126 CH OCH 2,4-di-FQ-126 CH OCH 4-CI
Q-130 CH OCH 4-F Q-130 CH OCH 2,4-di-FQ-130 CH OCH 4-Cl
Q-144 CH OCH 4-F Q-144 CH OCH 2,4-di-FQ-144 CH OCH 4-CI
Q-162 CH OCH 4-F Q-162 CH OCH 2,4-di-FQ-162 CH OCH 4-Cl
Q-169 CH20CH 4-F Q-169 CH OCH 2,4-di-FQ-169 CH OCH 4-Cl
Q-2 CH CF 4-F Q-2 CH CF 2,4-di-FQ-2 CH CF 4-Cl
Q-16 CH CF 4-F Q-16 CH CF 2,4-di-FQ-16 CH CF 4-Cl
Q-24 CH CF 4-F Q-24 CH CF 2,4-di-FQ-24 CH CF 4-Cl
Q-29 CH CF 4-F Q-29 CH CF 2,4-di-FQ-29 CH CF 4-CI
Q-57 CH CF 4-F Q-57 CH CF 2,4-di-FQ-57 CH CF 4-Cl
Q-71 CH CF 4-F Q-71 CH CF 2,4-di-FQ-71 CH CF 4-Cl
Q-100 CH CF 4-F Q-100 CH CF 2,4-di-FQ-100 CH CF 4-Cl
Q-119 CH CF 4-F Q-119 CH2CF 2,4-di-FQ-119 CH CF 4-CI
Q-120 CH CF 4-F Q-120 CH CF 2,4-di-FQ-120 CH CF 4-CI
Q-126 CH CF 4-F Q-126 CH CF 2,4-di-FQ-126 CH CF 4-CI
Q-130 CH CF 4-F Q-130 CH CF 2,4-di-FQ-130 CH CF 4-Cl
Q-144 CH CF 4-F Q-144 CH CF 2,4-di-FQ-144 CH CF 4-CI
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Q R2 R13 Q R2 R13 Q R2 R13
Q-162 CH CF 4-F Q-162 CH CF 2,4-di-FQ-162 CH CF 4-C1
Q-169 CH CF 4-F Q-169 CH CF3 2,4-di-FQ-169 CH CF 4-Cl
TABLE 2
O O
Qw ~ R1
N~
O R2
O
R1 is C2HS, R2 is B-1
Q Q Q Q Q Q Q Q Q
Q-1 Q'2 Q'3 Q-4 Q_5 Q_6 Q-7 Q_8 Q-9
Q-10 Q-11 Q-12 Q-13 Q-14 Q-15 Q-16 Q-17 Q-18
Q-19 Q-20 Q-21 Q-22 Q-23 Q-24 Q-25 Q-26 Q-27
Q-28 Q-29 Q-30 Q-31 Q-32 Q-33 Q-34 Q-35 Q-36
Q-37 Q-38 Q-39 Q-40 Q-41 Q-42 Q-43 Q-44 Q-45
Q-46 Q-47 Q-48 Q-49 Q-50 Q-51 Q-52 Q-53 Q-54
Q-55 Q-56 Q-57 Q-58 Q-59
Q-60 Q-61 Q-62 Q-63
Q-64 Q-65 Q-66 Q-67 Q-68 Q-69 Q-70 Q-71 Q-72
Q-73 Q-74 Q-75 Q-76 Q-77 Q-78 Q-79 Q-80 Q-81
Q-82 Q-83 Q-84 Q-85 Q-86 Q-87 Q-88 Q-89 Q-90
Q-91 Q-92 Q-93 Q-94 Q-95 Q-96 Q-97 Q-98 Q-99
Q-100 Q-101 Q-102 Q-103 Q-104 Q-105 Q-106 Q-107 Q-108
Q-109 Q-110 Q-111 Q-112 Q-113 Q-114 Q-115 Q-116
Q-117
Q-118 Q-119 Q-120 Q-121 Q-122 Q-123 Q-124 Q-125 Q-126
Q-127 Q-128 Q-129 Q-130 Q-131 Q-132 Q-133 Q-134 Q-135
Q-136 Q-137 Q-138 Q-139 Q-140 Q-141 Q-142 Q-143 Q-144
Q-145 Q-146 Q-147 Q-148 Q-149 Q-150 Q-151 Q-152 Q-153
Q-154 Q-155 Q-156 Q-157 Q-158 Q-159 Q-160 Q-161 Q-162
Q-163 Q-164 Q-165 Q-166 Q-167 Q-168 Q-169 Q-170 Q-171
Q-172 Q-173 Q-174 Q-175
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R1 is i-C~H7, R2 is B-4
Q Q Q Q Q Q Q Q Q
Q-1 Q-2 Q-3 Q-4 Q_5 Q_6 Q_7 Q_8 Q_9
Q-10 Q-11 Q-12 Q-13 Q-14 Q-15 Q-16 Q-17 Q-18
Q-19 Q-20 Q-21 Q-22 Q-23 Q-24 Q-25 Q-26 Q-27
Q-28 Q-29 Q-30 Q-31 Q-32 Q-33 Q-34 Q-35 Q-36
Q-37 Q-38 Q-39 Q-40 Q-41 Q-42 Q-43 Q-44 Q-45
Q-46 Q-47 Q-48 Q-49 Q-50 Q-51 Q-52 Q-53 Q-54
Q-55 Q-56 Q-57 Q-58 Q-59 Q-60 Q-61 Q-62 Q-63
Q-64 Q-65 Q-66 Q-67 Q-68 Q-69 Q-70 Q-71 Q-72
Q-73 Q-74 Q-75 Q-76 Q-77 Q-78 Q-79 Q-80 Q-81
Q-82 Q-83 Q-84 Q-85 Q-86 Q-87 Q-88 Q-89 Q-90
Q-91 Q-92 Q-93 Q-94 Q-95 Q-96 Q-97 Q-98 Q-99
Q-100 Q-101 Q-102 Q-103 Q-104 Q-105 Q-106 Q-107 Q-108
Q-109 Q-110 Q-111 Q-112 Q-113 Q-114 Q-115 Q-116 Q-117
Q-118 Q-119 Q-120 Q-121 Q-122 Q-123 Q-124 Q-125 Q-126
Q-127 Q-128 Q-129 Q-130 Q-131 Q-132
Q-133 Q-134 Q-135
Q-136 Q-137 Q-138 Q-139 Q-140 Q-141 Q-142 Q-143 Q-144
Q-145 Q-146 Q-147 Q-148 Q-149 Q-150 Q-151 Q-152 Q-153
Q-154 Q-155 Q-156 Q-157 Q-158 Q-159 Q-160 Q-161 Q-162
Q-163 Q-164 Q-165 Q-166 Q-167 Q-168 Q-169 Q-170 Q-171
Q-172 Q-173 Q-174 Q-175
R1 is C2H5, R2 is B-4
Q Q Q Q Q Q Q Q Q
Q-1 Q-2 Q-3 Q-4 Q_5 Q_6 Q_7 Q_8 Q_9
Q-10 Q-11 Q-12 Q-13 Q-14 Q-15 Q-16 Q-17 Q-18
Q-19 Q-20 Q-21 Q-22 Q-23 Q-24 Q-25 Q-26 Q-27
Q-28 Q-29 Q-30 Q-31 Q-32 Q-33 Q-34 Q-35 Q-36
Q-37 Q-38 Q-39 Q-40 Q-41 Q-42 Q-43 Q-44 Q-45
Q-46 Q-47 Q-48 Q-49 Q-50 Q-51 Q-52 Q-53 Q-54
Q-55 Q-56 Q-57 Q-58 Q-59 Q-60 Q-61 Q-62 Q-63
Q-64 Q-65 Q-66 Q-67 Q-68 Q-69 Q-70 Q-71 Q-72
Q-73 Q-74 Q-75 Q-76 Q-77 Q-78 Q-79 Q-80 Q-81
Q-82 Q-83 Q-84 Q-85 Q-86 Q-87 Q-88 Q-89 Q-90
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Q-91 Q-92 Q-93 Q-94 Q-95 Q-96 Q-97 Q-98 Q-99
Q-100 Q-101 Q-102 Q-103 Q-104 Q-105 Q-106 Q-107 Q-108
Q-109 Q-110 Q-111 Q-112 Q-113 Q-114 Q-115 Q-116 Q-117
Q-118 Q-119 Q-120 Q-121 Q-122 Q-123 Q-124
Q-125 Q-126
Q-127 Q-128 Q-129 Q-130 Q-131 Q-132 Q-133 Q-134 Q-135
Q-136 Q-137 Q-138 Q-139 Q-140 Q-141 Q-142 Q-143 Q-144
Q-145 Q-146 Q-147 Q-148 Q-149
Q-150 Q-151 Q-152 Q-153
Q-154 Q-155 Q-156 Q-157 Q-158 Q-159 Q-160 Q-161 Q-162
Q-163 Q-164 Q-165 Q-166 Q-167 Q-168 Q-169 Q-170 Q-171
Q-172 Q-173 Q-174 Q-175
R1 is C2H5, R2 is B-10
Q Q Q Q Q Q Q Q Q
Q-1 Q-2 Q-3 Q-4 Q_5 Q_6 Q_7 Q_8 Q_9
Q-10 Q-11 Q-12 Q-13 Q-14 Q-15 Q-16 Q-17 Q-18
Q-19 Q-20 Q-21 Q-22 Q-23 Q-24 Q-25 Q-26 Q-27
Q-28 Q-29 Q-30 Q-31 Q-32 Q-33 Q-34 Q-35 Q-36
Q-37 Q-38 Q-39 Q-40 Q-41 Q-42 Q-43 Q-44 Q-45
Q-46 Q-47 Q-48 Q-49 Q-50 Q-51
Q-52 Q-53 Q-54
Q-55 Q-56 Q-57 Q-58 Q-59 Q-60 Q-61 Q-62 Q-63
Q-64 Q-65 Q-66 Q-67 Q-68 Q-69 Q-70 Q-71 Q-72
Q-73 Q-74 Q-75 Q-76 Q-77 Q-78 Q-79 Q-80 Q-81
Q-82 Q-83 Q-84 Q-85 Q-86 Q-87 Q-88 Q-89 Q-90
Q-91 Q-92 Q-93 Q-94 Q-95 Q-96 Q-97 Q-98 Q-99
Q-100 Q-101 Q-102 Q-103 Q-104 Q-105 Q-106 Q-107 Q-108
Q-109 Q-110 Q-111 Q-112 Q-113 Q-114 Q-115 Q-116 Q-117
Q-118 Q-119 Q-120 Q-121 Q-122 Q-123 Q-124 Q-125 Q-126
Q-127 Q-128 Q-129 Q-130 Q-131 Q-132
Q-133 Q-134 Q-135
Q-136 Q-137 Q-138 Q-139 Q-140 Q-141 Q-142 Q-143 Q-144
Q-145 Q-146 Q-147 Q-148 Q-149 Q-150 Q-151 Q-152 Q-153
Q-154 Q-155 Q-156 Q-157 Q-158 Q-159 Q-160 Q-161 Q-162
Q-163 Q-164 Q-165 Q-166 Q-167 Q-168 Q-169 Q-170 Q-171
Q-172 Q-173 Q-174 Q-175
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R1 is i-C3H7, R2 is B-10
Q Q Q Q Q Q Q Q Q
Q-1 Q-2 Q-3 Q-4 Q_5 Q_6 Q-7 Q-8 Q_9
Q-10 Q-11 Q-12 Q-13 Q-14 Q-15 Q-16 Q-17 Q-18
Q-19 Q-20 Q-21 Q-22 Q-23 Q-24 Q-25 Q-26 Q-27
Q-28 Q-29 Q-30 Q-31 Q-32 Q-33 Q-34 Q-35 Q-36
Q-37 Q-38 Q-39 Q-40 Q-41 Q-42 Q-43 Q-44 Q-45
Q-46 Q-47 Q-48 Q-49 Q-50 Q-51 Q-52 Q-53 Q-54
Q-55 Q-56 Q-57 Q-58 Q-59 Q-60 Q-61 Q-62 Q-63
Q-64 Q-65 Q-66 Q-67 Q-68 Q-69 Q-70 Q-71 Q-72
Q-73 Q-74 Q-75 Q-76 Q-77 Q-78 Q-79 Q-80 Q-81
Q-82 Q-83 Q-84 Q-85 Q-86 Q-87 Q-88 Q-89 Q-90
Q-91 Q-92 Q-93 Q-94 Q-95 Q-96 Q-97 Q-98 Q-99
Q-100 Q-101 Q-102 Q-103 Q-104 Q-105 Q-106 Q-107 Q-108
Q-109 Q-110 Q-111 Q-112 Q-113 Q-114 Q-115 Q-116 Q-117
Q-118 Q-119 Q-120 Q-121 Q-122 Q-123 Q-124 Q-125 Q-126
Q-127 Q-128 Q-129 Q-130 Q-131 Q-132 Q-133 Q-134 Q-135
Q-136 Q-137 Q-138 Q-139 Q-140 Q-141 Q-142 Q-143 Q-144
Q-145 Q-146 Q-147 Q-148 Q-149 Q-150 Q-151 Q-152 Q-153
Q-154 Q-155 Q-156 Q-157 Q-158 Q-159 Q-160 Q-161 Q-162
Q-163 Q-164 Q-165 Q-166 Q-167 Q-168 Q-169 Q-170 Q-171
Q-172 Q-173 Q-174 Q-175
Q R1 R2 Q R1 R2 Q R1 R2
Q-2 CyclopropylB-10Q-2 Allyl B-4 Q-2 CyclohexylB-18
Q-16 CyclopropylB-10Q-16 Allyl B-4 Q-16 CyclohexylB-18
Q-24 CyclopropylB-10Q-24 Allyl B-4 Q-24 CyclohexylB-18
Q-29 CyclopropylB-10Q-29 Allyl B-4 Q-29 CyclohexylB-18
Q-57 CyclopropylB-10Q-57 Allyl B-4 Q-57 CyclohexylB-18
Q-71 CyclopropylB-10Q-71 Allyl B-4 Q-71 CyclohexylB-18
Q-100CyclopropylB-10Q-100 Allyl B-4 Q-100 CyclohexylB-18
Q-119CyclopropylB-10Q-119 Allyl B-4 Q-119 CyclohexylB-18
Q-120CyclopropylB-10Q-120 Allyl B-4 Q-120 CyclohexylB-18
Q-126CyclopropylB-10Q-126 Allyl B-4 Q-126 CyclohexylB-18
Q-130CyclopropylB-10Q-130 Allyl B-4 Q-130 CyclohexylB-18
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Q-144 CyclopropylB-10Q-144 Allyl B-4 Q-144 CyclohexylB-18
Q-162 CyclopropylB-10Q-162 Allyl B-4 Q-162 CyclohexylB-18
Q-169 CyclopropylB-10Q-169 Allyl B-4 Q-169 CyclohexylB-18
Q-2 n-C4H B-10Q-2 CyclopropylB-4 Q-2 i-C B-18
H
Q-16 n-C H B-10Q-16 CyclopropylB-4 Q-16 i-C B-18
H
Q-24 n-C H B-10Q-24 CyclopropylB-4 Q-24 i-C B-18
H
Q-29 n-C H B-10Q-29 CyclopropylB-4 Q-29 i-C B-18
H
Q-57 n-C H B-10Q-57 CyclopropylB-4 Q-57 i-C B-18
H
Q-71 n-C H B-10Q-71 CyclopropylB-4 Q-71 i-C B-18
H
Q-100 n-C H B-10Q-100 CyclopropylB-4 Q-100 i-C B-18
H
Q-119 n-C H B-10Q-119 CyclopropylB-4 Q-119 i-C H-18
H
Q-120 n-C4H B-10Q-120 CyclopropylB-4 Q-120 i-C B-18
H
Q-126 n-C H B-10Q-126 CyclopropylB-4 Q-126 i-C B-18
H
Q-130 n-C H B-10Q-130 CyclopropylB-4 Q-130 i-C B-18
H
Q-144 n-C H B-10Q-144 CyclopropylB-4 Q-144 i-C B-18
H
Q-162 n-C H B-10Q-162 CyclopropylB-4 Q-162 i-C B-18
H
Q-169 n-C H B-10Q-169 CyclopropylB-4 Q-169 i-C B-18
H
Q-2 CH CH OCH B-10Q-2 CH B-4 Q-2 CyclohexylB-17
Q-16 CH CH OCH B-10Q-16 CH B-4 Q-16 CyclohexylB-17
Q-24 CH CH OCH B-10Q-24 CH B-4 Q-24 CyclohexylB-17
Q-29 CH CH OCH B-10Q-29 CH B-4 Q-29 CyclohexylB-17
Q-57 CH CH OCH B-10Q-57 CH B-4 Q-57 CyclohexylB-17
Q-71 CH CH OCH B-10Q-71 CH B-4 Q-71 CyclohexylB-17
Q-100 CH CH OCH B-10Q-100 CH B-4 Q-100 CyclohexylB-17
Q-119 CH CH OCH B-10Q-119 CH B-4 Q-119 CyclohexylB-17
Q-120 CH CH OCH B-10Q-120 CH B-4 Q-120 CyclohexylB-17
Q-126 CH CH OCH B-10Q-126 CH B-4 Q-126 CyclohexylB-17
Q-130 CH CH OCH B-10Q-130 CH B-4 Q-130 CyclohexylB-17
Q-144 CH CH OCH B-10Q-144 CH B-4 Q-144 CyclohexylB-17
Q-162 CH CH OCH B-10Q-162 CH B-4 Q-162 CyclohexylB-17
Q-169 CH CH OCH B-10Q-169 CH B-4 Q-169 CyclohexylB-17
Q-2 CH B-10Q-2 CH B-4 Q-2 C H B-17
Q-16 CH B-10Q-16 CH B-4 Q-16 C H B-17
Q-24 CH3 I B-10Q-24 CH B-4 Q-24 C2H5 B-17
I I I
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Q-29 CH B-10 Q-29 CH B-4 Q-29 C H B-17
Q-57 CH B-10 Q-57 CH B-4 Q-57 C H B-17
Q-71 CH B-10 Q-71 CH B-4 Q-71 C H B-17
Q-100CH B-10 Q-100 CH3 B-4 Q-100 C H B-17
Q-119CH B-10 Q-119 CH B-4 Q-119 C H B-17
Q-120CH B-10 Q-120 CH B-4 Q-120 C H B-17
Q-126CH B-10 Q-126 CH B-4 Q-126 C H B-17
Q-130CH B-10 Q-130 CH B-4 Q-130 C H B-17
Q-144CH B-10 Q-144 CH B-4 Q-144 C H B-17
Q-162CH B-10 Q-162 CH B-4 Q-162 C H B-17
Q-169CH B-10 Q-169 CH B-4 Q-169 C H B-17
Q-2 n-C H B-10 Q-2 CH CF B-4 Q-2 n-C H B-6
Q-16 n-C H B-10 Q-16 CH CF B-4 Q-16 n-C H B-6
Q-24 n-C H B-10 Q-24 CH CF B-4 Q-24 n-C H B-6
Q-29 n-C H B-10 Q-29 CH CF B-4 Q-29 n-C H B-6
Q-57 n-C H B-10 Q-57 CH CF B-4 Q-57 n-C H B-6
Q-71 n-C H B-10 Q-71 CH CF B-4 Q-71 n-C H B-6
Q-100n-C H B-10 Q-100 CH CF B-4 Q-100 n-C H B-6
Q-119n-C H B-10 Q-119 CH CF B-4 Q-119 n-C H B-6
Q-120n-C H B-10 Q-120 CH CF B-4 Q-120 n-C H B-6
Q-126n-C H B-10 Q-126 CH CF B-4 Q-126 n-C H B-6
Q-130n-C H B-10 Q-130 CH CF B-4 Q-130 n-C H B-6
Q-144n-C H B-10 Q-144 CH CF B-4 Q-144 n-C H B-6
Q-162n-C H B-10 Q-162 CH2CF B-4 Q-162 n-C H B-6
Q-169n-C H B-10 Q-169 CH CF B-4 Q-169 n-C H B-6
Q R1 R2 Q R1 R2 Q RI R2
Q-2 C H B-2 Q-2 C H B-5 Q-2 C H B-8
Q-16 C H B-2 Q-16 C H B-5 Q-16 C H B-8
Q-24 C H B-2 Q-24 C H B-5 Q-24 C H B-8
Q-29 C H B-2 Q-29 C H B-5 Q-29 C H B-8
Q-57 C H B-2 Q-57 C H B-5 Q-57 C H B-8
Q-71 C H B-2 Q-71 C H B-5 Q-71 C H B-8
Q-100 C H B-2 Q-100 C H B-5 Q-100 C H B-8
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Q-119 C H B-2 Q-119 C H B-5 Q-119 C H B-8
Q-120 C H B-2 Q-120 C H B-5 Q-120 C H B-8
Q-126 C H B-2 Q-126 C H B-5 Q-126 C H B-8
Q-130 C2H B-2 Q-130 C H B-5 Q-130 C H B-8
Q-144 C H B-2 Q-144 C H B-5 Q-144 C H B-8
Q-162 C H B-2 Q-162 C H B-5 Q-162 C H B-8
Q-169 C H B-2 Q-169 C H B-5 Q-169 C H B-8
Q-2 C H B-2 Q-2 i-C H B-6 Q-2 CyclopropylB-8
Q-16 C H B-2 Q-16 i-C H B-6 Q-16 CyclopropylB-8
Q-24 C H B-2 Q-24 i-C H B-6 Q-24 CyclopropylB-8
Q-29 C H B-2 Q-29 i-C H B-6 Q-29 CyclopropylB-8
Q-57 C H7 B-2 Q-57 i-C H B-6 Q-57 CyclopropylB-8
Q-71 C H B-2 Q-71 i-C H B-6 Q-71 CyclopropylB-8
Q-100 C H B-2 Q-100 i-C H B-6 Q-100 CyclopropylB-8
Q-119 C H B-2 Q-119 i-C H B-6 Q-119 CyclopropylB-8
Q-120 C H B-2 Q-120 i-C H B-6 Q-120 CyclopropylB-8
Q-126 C H B-2 Q-126 i-C H B-6 Q-126 CyclopropylB-8
Q-130 C H B-2 Q-130 i-C H B-6 Q-130 CyclopropylB-8
Q-144 C H B-2 Q-144 i-C H B-6 Q-144 CyclopropylB-8
Q-162 C H B-2 Q-162 i-C H B-6 Q-162 CyclopropylB-8
Q-169 C H B-2 Q-169 i-C H B-6 Q-169 CyclopropylB-8
Q-2 C H B-3 Q-2 C H B-6 Q-2 C H B-9
Q-16 C H B-3 Q-16 C H B-6 Q-16 C H B-9
Q-24 C H B-3 Q-24 C H B-6 Q-24 C H B-9
Q-29 C H B-3 Q-29 C H B-6 Q-29 C H B-9
Q-57 C H B-3 Q-57 C H B-6 Q-57 C H B-9
Q-71 C H B-3 Q-71 C H B-6 Q-71 C H B-9
Q-100 C H B-3 Q-100 C H B-6 Q-100 C H B-9
Q-119 C H B-3 Q-119 C H B-6 Q-119 C H B-9
Q-120 C H B-3 Q-120 C H B-6 Q-120 C H B-9
Q-126 C H B-3 Q-126 C H B-6 Q-126 C H B-9
Q-130 C H B-3 Q-130 C H B-6 Q-130 C H B-9
Q-144 C H B-3 Q-144 C H B-6 Q-144 C H B-9
Q-162 C H B-3 Q-162 C H B-6 Q-162 C H B-9
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Q-169 C H B-3 Q-169 C H B-6 Q-169 C H B-9
Q-2 i-C H B-3 Q-2 C H B-7 Q-2 i-C H B-9
Q-16 i-C H B-3 Q-16 C H B-7 Q-16 i-C H B-9
Q-24 i-C H B-3 Q-24 C2H B-7 Q-24 i-C H B-9
Q-29 i-C H B-3 Q-29 C H B-7 Q-29 i-C H B-9
Q-57 i-C H B-3 Q-57 C H B-7 Q-57 i-C H B-9
Q-71 i-C H B-3 Q-71 C H B-7 Q-71 i-C H B-9
Q-100 i-C H B-3 Q-100 C H B-7 Q-100 i-C H B-9
Q-119 i-C H B-3 Q-119 C H B-7 Q-119 i-C H B-9
Q-120 i-C H B-3 Q-120 C H B-7 Q-120 i-C H B-9
Q-126 i-C H B-3 Q-126 C H B-7 Q-126 i-C H B-9
Q-130 i-C H B-3 Q-130 C2H B-7 Q-130 i-C H B-9
Q-144 i-C H B-3 Q-144 C H B-7 Q-144 i-C H B-9
Q-162 i-C H B-3 Q-162 C H B-7 Q-162 i-C H B-9
Q-169 i-C H B-3 Q-169 C H B-7 Q-169 i-C H B-9
Q-2 C H B-4 Q-2 i-C H B-7 Q-2 C H B-11
Q-16 C H B-4 Q-16 i-C H B-7 Q-16 C H B-11
Q-24 C H B-4 Q-24 i-C H B-7 Q-24 C H B-11
Q-29 C H B-4 Q-29 i-C H B-7 Q-29 C H B-11
Q-57 C H B-4 Q-57 i-C H B-7 Q-57 C H B-11
Q-71 C H B-4 Q-71 i-C H B-7 Q-71 C H B-11
Q-100 C H B-4 Q-100 i-C H B-7 Q-100 C H B-11
Q-119 C H B-4 Q-119 i-C H B-7 Q-119 C H B-11
Q-120 C H B-4 Q-120 i-C H B-7 Q-120 C H B-11
Q-126 C H B-4 Q-126 i-C H B-7 Q-126 C H B-11
Q-130 C H B-4 Q-130 i-C H B-7 Q-130 C H B-11
Q-144 C H B-4 Q-144 i-C H B-? Q-144 C H B-11
Q-162 C2H B-4 Q-162 i-C H7 B-7 Q-162 C2H B-11
Q-169 C H B-4 Q-169 i-C H B-7 Q-169 C H B-11
Q RI R2 Q RI R2 Q RI R2
Q-2 CyciopropylB-11 Q-2 C H B-14 Q-2 i-C H B-16
Q-16 CyclopropylB-11 Q-16 C H B-14 Q-16 i-C H B-16
Q-24 CyclopropylB-11 Q-24 C H B-14 Q-24 i-C H B-16
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Q-29 CyclopropylB-11 Q-29 C H B-14 Q-29 i-C H B-16
Q-57 CyclopropylB-11 Q-57 C H B-14 Q-57 i-C H B-16
Q-71 CyclopropylB-11 Q-71 C H B-14 Q-71 i-C H B-16
Q-100 CyclopropylB-11 Q-100 C H B-14 Q-100 i-C H B-16
Q-119 CyclopropylB-11 Q-119 C H B-14 Q-119 i-C H B-16
Q-120 CyclopropylB-11 Q-120 C H B-14 Q-120 i-C H B-16
Q-126 CyclopropylB-11 Q-126 C H B-14 Q-126 i-C H B-16
Q-130 CyclopropylB-11 Q-130 C H B-14 Q-130 i-C H B-16
Q-144 CyclopropylB-11 Q-144 C H B-14 Q-144 i-C H B-16
Q-162 CyclopropylB-11 Q-162 C H B-14 Q-162 i-C H B-16
Q-169 CyclopropylB-11 Q-169 C H B-14 Q-169 i-C H B-16
Q-2 C H B-12 Q-2 i-C H B-14 Q-2 t-C H B-10
Q-16 C H B-12 Q-16 i-C H B-14 Q-16 t-C H B-10
Q-24 C H B-12 Q-24 i-C H B-14 Q-24 t-C H B-10
Q-29 C H B-12 Q-29 i-C H B-14 Q-29 t-C H B-10
Q-57 C H B-12 Q-57 i-C H B-14 Q-57 t-C4H B-10
Q-71 C H B-12 Q-71 i-C H B-14 Q-71 t-C H B-10
Q-100 C H B-12 Q-100 i-C H B-14 Q-100 t-C H B-10
Q-119 C H B-12 Q-119 i-C H B-14 Q-119 t-C H B-10
Q-120 C2H B-12 Q-120 i-C H B-14 Q-120 t-C H B-10
Q-126 C H B-12 Q-126 i-C H B-14 Q-126 t-C H B-10
Q-130 C H B-12 Q-130 i-C H B-14 Q-130 t-C H B-10
Q-144 C H B-12 Q-144 i-C H B-14 Q-144 t-C H B-10
Q-162 C H B-12 Q-162 i-C H B-14 Q-162 t-C4H B-10
Q-169 C H B-12 Q-169 i-C H B-14 Q-169 t-C H B-10
Q-2 i-C B-12 Q-2 C H B-15 Q-2 i-C H B-10
H
Q-16 i-C B-12 Q-16 C H B-15 Q-16 i-C H B-10
H
Q-24 i-C B-12 Q-24 C H B-15 Q-24 i-C H B-10
H
Q-29 i-C B-12 Q-29 C H B-15 Q-29 i-C H B-10
H
Q-57 i-C B-12 Q-57 C H B-15 Q-57 i-C H B-10
H
Q-71 i-C B-12 Q-71 C H B-15 Q-71 i-C H B-10
H
Q-100 i-C B-12 Q-100 C H B-15 Q-100 i-C H B-10
H
Q-119 i-C B-12 Q-119 C H B-15 Q-119 i-C H B-10
H
Q-120 i-C B-12 Q-120 C H B-15 Q-120 i-C H B-10
H
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Q-126 i-C H B-12Q-126 C H B-15 Q-126 i-C H B-10
Q-130 i-C H B-12Q-130 C H B-15 Q-130 i-C H B-10
Q-144 i-C H B-12Q-144 C H B-15 Q-144 i-C H B-10
Q-162 i-C H B-12Q-162 C H B-15 Q-162 i-C H B-10
Q-169 i-C H B-12Q-169 C H B-15 Q-169 i-C H B-10
Q-2 C H B-13Q-2 i-C H B-15 Q-2 CH CF B-10
Q-16 C H B-13Q-16 i-C H B-15 Q-16 CH CF B-10
Q-24 C H B-13Q-24 i-C H B-15 Q-24 CH CF B-10
Q-29 C H B-13Q-29 i-C H B-15 Q-29 CH CF B-10
Q-57 C H B-13Q-57 i-C H B-15 Q-57 CH CF B-10
Q-71 C H B-13Q-71 i-C H B-15 Q-71 CH CF B-10
Q-100 C2H B-13Q-100 i-C H B-15 Q-100 CH CF B-10
Q-119 C H B-13Q-119 i-C H B-15 Q-119 CH CF B-10
Q-120 C H B-13Q-120 i-C H B-15 Q-120 CH CF B-10
Q-126 C H B-13Q-126 i-C H B-15 Q-126 CH CF B-10
Q-130 C2H B-13Q-130 i-C H B-15 Q-130 CH CF B-10
Q-144 C H B-13Q-144 i-C H B-15 Q-144 CH CF B-10
Q-162 C H B-13Q-162 i-C H B-15 Q-162 CH CF B-10
Q-169 C H B-13Q-169 i-C H B-15 Q-169 CH CF B-10
Q-2 i-C H B-13Q-2 C H B-16 Q-2 n-C H B-10
Q-16 i-C H B-13Q-16 C H B-16 Q-16 n-C H B-10
Q-24 i-C H B-13Q-24 C H B-16 Q-24 n-C H B-10
Q-29 i-C H B-13Q-29 C H B-16 Q-29 n-C H B-10
Q-57 i-C H7 B-13Q-57 C H B-16 Q-57 n-C H B-10
Q-71 i-C H B-13Q-71 C H B-16 Q-71 n-C H B-10
Q-100 i-C H B-13Q-100 C H B-16 Q-100 n-C H B-10
Q-119 i-C H B-13Q-119 C H B-16 Q-119 n-C H B-10
Q-120 i-C H B-13Q-120 C H B-16 Q-120 n-C H B-10
Q-126 i-C H B-13Q-126 C H B-16 Q-126 n-C H B-10
Q-130 i-C H B-13Q-130 C H B-16 Q-130 n-C H B-10
Q-144 i-C H B-13Q-144 C H B-16 Q-144 n-C H B-10
Q-162 i-C H B-13Q-162 C H B-16 Q-162 n-C H B-10
Q-169 i-C H B-13Q-169 C H B-16 Q-169 n-C H B-10
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TABLE 3
X2 X3
Rl
N~
1~ p R2
X
Q X' Xs X3 R' RZ
i-Pr S O O i-Pr 4-F-Phenyl
i-Pr O S O i-Pr 4-F-Phenyl
i-Pr O O S i-Pr 4-F-Phenyl
i-Pr NMe O O i-Pr 4-F-Phenyl
i-Pr O NMe O i-Pr 4-F-Phenyl
i-Pr O O NMe i-Pr 4-F-Phenyl
i-Pr NCN O O i-Pr 4-F-Phenyl
i-Pr O NCN O i-Pr 4-F-Phenyl
i-Pr O O NCN i-Pr 4-F-Phenyl
i-Pr S S O i-Pr 4-F-Phenyl
i-Pr S O S i-Pr 4-F-Phenyl
i-Pr O S S i-Pr 4-F-Phenyl
i-Pr S S S i-Pr 4-F-Phenyl
c-Pr S O O i-Pr 4-F-Phenyl
c-Pr O S O i-Pr 4-F-Phenyl
c-Pr O O S i-Pr 4-F-Phenyl
c-Pr NMe O O i-Pr 4-F-Phenyl
c-Pr O NMe O i-Pr 4-F-Phenyl
c-Pr O O NMe i-Pr 4-F-Phenyl
c-Pr NCN O O i-Pr 4-F-Phenyl
c-Pr O NCN O i-Pr 4-F-Phenyl
c-Pr O O NCN i-Pr 4-F-Phenyl
c-Pr S S O i-Pr 4-F-Phenyl
c-Pr S O S i-Pr 4-F-Phenyl
c-Pr O S S i-Pr 4-F-Phenyl
c-Pr S S S i-Pr 4-F-Phenyl
i-Pr O O O i-Pr 2-C1-Pyridin-5-yl
i-Pr O O O i-Pr 2-F-Pyridin-5-yl
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i-Pr O O O i-Pr 2-Br-Pyridin-5-yl
i-Pr O O O i-Pr 2-Me-Pyridin-5-yl
i-Pr O O O i-Pr 2-CF3-Pyridin-5-yl
i-Pr O O O i-Pr 2-CI-Pyrimidin-5-yl
i-Pr O O O i-Pr 2-F-Pyrimidin-5-yl
i-Pr O O O i-Pr 2-Br-Pyrimidin-5-yl
i-Pr O O O i-Pr 2-Me-Pyrimidin-5-yl
i-Pr O O O i-Pr 2-CF3-Pyrimidin-5-yl
i-Pr O O O i-Pr 2-CI-Thien-5-yl
i-Pr O O O i-Pr 2-F-Thien-5-yl
i-Pr O O O i-Pr 2-Me-Thien-5-yl
i-Pr O O O i-Pr Thien-2-yl
i-Pr O O O i-Pr Pyrimidin-5-yl
i-Pr O O O i-Pr 2-Cl-Pyridazin-5-yl
i-Pr O O O i-Pr 2-Cl-1,3,4-Thiadiazol-5-yl
i-Pr O O O i-Pr 2-CF3-1,3,4-Thiadiazol-5-yl
i-Pr O O O i-Pr 2-CI-Thiazol-5-yl
i-Pr O O O i-Pr 5-Cl-Thiazol-2-yl
c-Pr O O O i-Pr Thien-2-yl
Et O O O i-Pr Thien-2-yl
n-Pr O O O i-Pr Thien-2-yl
Me O O O i-Pr Thien-2-yl
i-Bu O O O i-Pr Thien-2-yl
Allyl O O O i-Pr Thien-2-yl
c-HexylO O O i-Pr Thien-2-yl
c-Pr O O O i-Pr 2-Cl-Pyridin-5-yl
Et O O O i-Pr 2-Cl-Pyridin-5-yl
n-Pr O O O i-Pr 2-CI-Pyridin-5-yl
Me O O O i-Pr 2-CI-Pyridin-5-yl
i-Bu O O O i-Pr 2-Cl-Pyridin-5-yl
Allyl O O O i-Pr 2-Cl-Pyridin-5-yl
c-HexylO O O i-Pr 2-Cl-Pyridin-5-yl
s-Bu O O O i-Pr 2-CI-Pyridin-5-yl
s-Bu O O O i-Pr Thien-2-yl
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Formulation/Utility
Compounds of this invention will generally be used as a formulation or
composition
with an agriculturally suitable carrier comprising at least one of a liquid
diluent, a solid
diluent or a surfactant. The formulation or composition ingredients are
selected to be
5 consistent with the physical properties of the active ingredient, mode of
application and
environmental factors such as soil type, moisture and temperature. Useful
formulations
include liquids such as solutions (including emulsifiable concentrates),
suspensions,
emulsions (including microemulsions and/or suspoemulsions) and the like which
optionally
can be thickened into gels. Useful formulations further include solids such as
dusts,
10 powders, granules, pellets, tablets, films, and the like which can be water-
dispersible
("wettable") or water-soluble. Active ingredient can be (micro)encapsulated
and further
formed into a suspension or solid formulation; alternatively the entire
formulation of active
ingredient can be encapsulated (or "overcoated"). Encapsulation can control or
delay release
of the active ingredient. Sprayable formulations can be extended in suitable
media and used
15 at spray volumes from about one to several hundred liters per hectare. High-
strength
compositions are primarily used as intermediates for fiwther formulation.
The formulations will typically contain effective amounts of active
ingredient,
diluent and surfactant within the following approximate ranges which add up to
100 percent
by weight.
Weight Percent
Active
In edient Diluent Surfactant
Water-Dispersible and 5-90 0-94 1-15
Water-soluble
Granules, Tablets and
Powders.
Suspensions, Emulsions,5-50 40-95 0-15
Solutions
(including Emulsifiable
Concentrates)
Dusts 1-25 70-99 0-5
Granules and Pellets 0.01-99 5-99.99 0-15
High Strength Compositions90-99 0-10 0-2
20 Typical solid diluents are described in Watkins, et al., Handbook of
Insecticide Dust
Diluents and Carriers, 2nd Ed., Dorland Books, Caldwell, New Jersey. Typical
liquid
diluents are described in Marsden, Solvents Guide, 2nd Ed., Interscience, New
York, 1950.
McCutcheon's Detergents and Emulsifiers Annual, Allured Publ. Corp.,
Ridgewood, New
Jersey, as well as Sisely and Wood, Encyclopedia of Surface Active Agents,
Chemical Publ.
25 Co., Inc., New York, 1964, list surfactants and recommended uses. All
formulations can
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contain minor amounts of additives to reduce foam, caking, corrosion,
microbiological
growth and the like, or thickeners to increase viscosity.
Surfactants include, for example, polyethoxylated alcohols, polyethoxylated
alkylphenols, polyethoxylated sorbitan fatty acid esters, dialkyl
sulfosuccinates, alkyl
sulfates, alkylbenzene sulfonates, organosilicones, N,N dialkyltaurates,
lignin sulfonates,
naphthalene sulfonate formaldehyde condensates, polycarboxylates, and
polyoxyethylene/polyoxypropylene block copolymers. Solid diluents include, for
example,
clays such as bentonite, montmorillonite, attapulgite and kaolin, starch,
sugar, silica, talc,
diatomaceous earth, urea, calcium carbonate, sodium carbonate and bicarbonate,
and sodium
sulfate. Liquid diluents include, for example, water, N,N dimethylformamide,
dimethyl
sulfoxide, N alkylpyrrolidone, ethylene glycol, polypropylene glycol,
paraffins,
alkylbenzenes, alkylnaphthalenes, oils of olive, castor, linseed, tong,
sesame, corn, peanut,
cotton-seed, soybean, rape-seed and coconut, fatty acid esters, ketones such
as
cyclohexanone, 2-heptanone, isophorone and 4-hydroxy-4-methyl-2-pentanone, and
alcohols
such as methanol, cyclohexanol, decanol and tetrahydrofurfuryl alcohol.
Solutions, including emulsifiable concentrates, can be prepared by simply
mixing the
ingredients. Dusts and powders can be prepared by blending and, usually,
grinding as in a
hammer mill or fluid-energy mill. Suspensions are usually prepared by wet-
milling; see, for
example, U.S. 3,060,084. Granules and pellets can be prepared by spraying the
active
material upon preformed granular Garners or by agglomeration techniques. See
Browning,
"Agglomeration", Chemical Engineering, December 4, 1967, pp 147-48, Perry's
Chemical
Engineer's Handbook, 4th Ed., McGraw-Hill, New York, 1963, pages 8-57 and
following,
and WO 91/13546. Pellets can be prepared as described in U.S. 4,172,714.
Water-dispersible and water-soluble granules can be prepared as taught in U.S.
4,144,050,
U.S. 3,920,442 and DE 3,246,493. Tablets can be prepared as taught in U.S.
5,180,587, U.S.
5,232,701 and U.S. 5,208,030. Finns can be prepared as taught in GB 2,095,558
and U.S.
3,299,566.
For further information regarding the art of formulation, see U.S. 3,235,361,
Col. 6,
line 16 through Col. 7, line 19 and Examples 10-41; U.S. 3,309,192, Col. 5,
line 43 through
Col. 7, line 62 and Examples 8, 12, 15, 39, 41, 52, 53, 58, 132, 138-140, 162-
164, 166, 167
and 169-182; U.S. 2,891,855, Col. 3, line 66 through Col. 5, line 17 and
Examples 1-4;
Klingman, Weed Control as a Science, John Wiley and Sons, Inc., New York,
1961,
pp 81-96; and Hance et al., Weed Control Handbook, 8th Ed., Blackwell
Scientific
Publications, Oxford, 1989.
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In the following Examples, all percentages are by weight and all formulations
are
prepared in conventional ways. Compound numbers refer to compounds in Index
Tables A-D below.
Example A
Hi~ Strength Concentrate
Compound 2 98.5%
silica aerogel 0.5%
synthetic amorphous fine silica 1.0%.
Example B
Wettable Powder
Compound 2 65.0%
dodecylphenol polyethylene glycol ether 2.0%
sodium ligninsulfonate 4.0%
sodium silicoaluminate 6.0%
montmorillonite (calcined) 23.0%.
Example C
Granule
Compound 2 10.0%
attapulgite granules (low volatile matter,
0.71/0.30 mm; U.S.S. No. 25-SO sieves) 90.0%.
Example D
Extruded Pellet
Compound 2 25.0%
anhydrous sodium sulfate 10.0%
crude calcium ligninsulfonate 5.0%
sodium alkylnaphthalenesulfonate 1.0%
calcium/magnesium bentonite 59.0%.
Test results indicate that the compounds of the present invention are highly
active
preemergent and postemergent herbicides or plant growth regulants. Many of
them have
utility for broad-spectrum pre- and/or postemergence weed control in areas
where complete
control of all vegetation is desired such as around fuel storage tanks,
industrial storage areas,
parking lots, drive-in theaters, air fields, river banks, irrigation and other
waterways, around
billboards and highway and railroad structures. Some of the compounds are
useful for the
control of selected grass and broadleaf weeds with tolerance to important
agronomic crops
which include but are not limited to alfalfa, barley, cotton, wheat, rape,
sugar beets, corn
(maize), sorghum, soybeans, rice, oats, peanuts, vegetables, tomato, potato,
perennial
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plantation crops including coffee, cocoa, oil palm, rubber, sugarcane, citrus,
grapes, fruit
trees, nut trees, banana, plantain, pineapple, hops, tea and forests such as
eucalyptus and
conifers (e.g., loblolly pine), and turf species (e.g., Kentucky bluegrass,
St. Augustine grass,
Kentucky fescue and Bermuda grass). Those skilled in the art will appreciate
that not all
compounds are equally effective against all weeds. Alternatively, the subject
compounds are
useful to modify plant growth.
A herbicidally effective amount of the compounds of this invention is
determined by
a number of factors. These factors include: formulation selected, method of
application,
amount and type of vegetation present, growing conditions, etc. In general, a
herbicidally
effective amount of compounds of this invention is 0.001 to 20 kg/ha with a
preferred range
of 0.004 to 1.0 kg/ha. One skilled in the art can easily determine the
herbicidally effective
amount necessary for the desired level of weed control.
Compounds of this invention can be used alone or in combination with other
commercial herbicides, insecticides or fungicides. Compounds of this invention
can also be
used in combination with commercial herbicide safeners such as benoxacor,
dichlormid and
furilazole to increase safety to certain crops. A mixture of one or more of
the following
herbicides with a compound of this invention may be particularly useful for
weed control:
acetochlor, acifluorfen and its sodium salt, aclonifen, acrolein (2-propenal),
alachlor,
ametryn, amidosulfuron, amitrole, ammonium sulfamate, anilofos, asulam,
atrazine,
azafenidin, azimsulfuron, benazolin, benazolin-ethyl, benfluralin,
benfuresate,
bensulfuron-methyl, bensulide, bentazone, bifenox, bispyribac and its sodium
salt, bromacil,
bromoxynil, bromoxynil octanoate, butachlor, butralin, butroxydim (ICIA0500),
butylate,
caloxydim (BAS 620H), carfentrazone-ethyl, chlomethoxyfen, chloramben,
chlorbromuron,
chloridazon, chlorimuron-ethyl, chlornitrofen, chlorotoluron, chlorpropham,
chlorsulfuron,
chlorthal-dimethyl, cinmethylin, cinosulfuron, clethodim, clomazone,
clopyralid,
clopyralid-olamine, cyanazine, cycloate, cyclosulfamuron, 2,4-D and its
butotyl, butyl,
isoctyl and isopropyl esters and its dimethylammonium, diolamine and trolamine
salts,
daimuron, dalapon, dalapon-sodium, dazomet, 2,4-DB and its dimethylammonium,
potassium and sodium salts, desmedipham, desmetryn, dicamba and its
diglycolammonium,
dimethylammonium, potassium and sodium salts, dichlobenil, dichlorprop,
diclofop-methyl,
2-[4,5-dihydro-4-methyl-4-(1-methylethyl)-5-oxo-1H imidazol-2-yl]-5-methyl-3-
pyridinecarboxylic acid (AC 263,222), difenzoquat metilsulfate, diflufenican,
dimepiperate,
dimethenamid, dimethylarsinic acid and its sodium salt, dinitramine,
diphenamid, diquat
dibromide, dithiopyr, diuron, DNOC, endothal, EPTC, esprocarb, ethalfluralin,
ethametsulfuron-methyl, ethofumesate, ethoxysulfuron, fenoxaprop-ethyl,
fenoxaprop-P-ethyl, fenuron, fenuron-TCA, flamprop-methyl, flamprop-M-
isopropyl,
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flamprop-M-methyl, flazasulfuron, fluazifop-butyl, fluazifop-P-butyl,
fluchloralin,
flufenacet, flumetsulam, flumiclorac-pentyl, flumioxazin, fluometuron,
fluoroglycofen-ethyl,
flupoxam, flupyrsulfuron-methyl and its sodium salt, fluridone,
flurochloridone, fluroxypyr,
fluthiacet-methyl, fomesafen, fosamine-ammonium, glufosinate, glufosinate-
ammonium,
glyphosate, glyphosate-isopropylammonium, glyphosate-sesquisodium,
glyphosate-trimesium, halosulfuron-methyl, haloxyfop-etotyl, haloxyfop-methyl,
hexazinone, imazamethabenz-methyl, imazamox, imazapyr, imazaquin,
imazaquin-ammonium, imazethapyr, imazethapyr-ammonium, imazosulfuron, ioxynil,
ioxynil octanoate, ioxynil-sodium, isoproturon, isouron, isoxaben,
isoxaflutole, lactofen,
lenacil, linuron, malefic hydrazide, MCPA and its dimethylammonium, potassium
and
sodium salts, MCPA-isoctyl, mecoprop, mecoprop-P, mefenacet, mefluidide,
metam-sodium, methabenzthiazuron, methylarsonic acid and its calcium,
monoammonium,
monosodium and disodium salts, methyl [[[1-[5-[2-chloro-4-
(trifluoromethyl)phenoxy]-2-
nitrophenyl]-2-methoxyethylidene]amino]oxy]acetate (AKH-7088), methyl 5-
[[[[(4,6-
dimethyl-2-pyrimidinyl)amino]carbonyl]amino]sulfonyl]-1-(2-pyridinyl)-1H
pyrazole-4-
carboxylate (NC-330), metobenzuron, metolachlor, metosulam, metoxuron,
metribuzin,
metsulfuron-methyl, molinate, monolinuron, napropamide, naptalam, neburon,
nicosulfuron,
norflurazon, oryzalin, oxadiazon, oxasulfuron, oxyfluorfen, paraquat
dichloride, pebulate,
pendimethalin, pentoxazone (KPP-314), perfluidone, phenmedipham, picloram,
picloram-potassium, pretilachlor, primisulfuron-methyl, prometon, prometryn,
propachlor,
propanil, propaquizafop, propazine, propham, propyzamide, prosulfuron,
pyrazolynate,
pyrazosulfuron-ethyl, pyridate, pyriminobac-methyl, pyrithiobac, pyrithiobac-
sodium,
quinclorac, quizalofop-ethyl, quizalofop-P-ethyl, quizalofop-P-tefuryl,
rimsulfuron,
sethoxydim, siduron, simazine, sulcotrione (ICIA0051 ), sulfentrazone,
sulfometuron-methyl,
TCA, TCA-sodium, tebuthiuron, terbacil, terbuthylazine, terbutryn,
thenylchlor,
thiafluamide (BAY 11390), thifensulfuron-methyl, thiobencarb, tralkoxydim, tri-
allate,
triasulfuron, triaziflam, tribenuron-methyl, triclopyr, triclopyr-butotyl,
triclopyr-triethylammonium, tridiphane, trifluralin, triflusulfuron-methyl,
and vernolate.
In certain instances, combinations with other herbicides having a similar
spectrum of
control but a different mode of action will be particularly advantageous for
preventing the
development of resistant weeds. Certain combinations of compounds of this
invention with
other herbicides may provide synergistic herbicidal effects on weeds or may
provide
enhanced crop safety.
Preferred for better control of undesired vegetation in corn (e.g., lower use
rate,
broader spectrum of weeds controlled, or enhanced crop safety) or for
preventing the
development of resistant weeds in corn are mixtures of a compound of this
invention with
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one or more of the herbicides selected from the group rimsulfuron,
nicosulfuron,
thifensulfuron, prosulfuron, halosulfuron, naphthalic anhydride, flurazole,
dichlormid,
fenchlorazole ethyl, naphthalic anhydride, MG-191 (2-dichloromethyl)-2-methyl-
1,3-
dioxolane), dicyclonon, benoxacor, cyometrinil, furilazole, oxabetrinil,
cloquintocet mexyl,
5 fluxofenim, fenclorim, menfenpyr diethyl, and R-29148 (3-(dichloroacetyl)-
2,2,5-
trimethyloxazolidine):
Specifically preferred mixtures for use in corn are selected from the group
consisting
of
a) Compound 113 (Index Table C, mixture partner A, generally applied at a rate
of 10
10 to 1000 g/ha, preferably applied at a rate of 50 to 500 g/ha) in
combination with:
Combination
Number Mixture partner B
1 rimsulfuron
2 nicosulfuron
3 dichlormid
4 benoxacor
5 naphthalic anhydride
6 rimsulfuron (B 1 ) in combination with dichlormid (B2)
7 nicosulfuron (B3) in combination with dichlormid (B4)
Combination 1 is generally used in a ratio of A to B of 3:1 to 50:1,
preferably 5:1 to
30:1, with B being applied at a rate of 1 to 100 g/ha, preferably S to SO
g/ha. Combination 2
15 is generally used in a ratio of A to B of 2:1 to 20:1, preferably 4:1 to
10:1, with B being
applied at a rate of 1 to 100 g/ha, preferably 20 to 70 g/ha. Combination 3 is
generally used
in a ratio of A to B of 1:10 to 10:1, preferably 1:2 to 2:1, with B being
applied at a rate of 10
to 1000 g/ha, preferably 50 to 500 g/ha. Combination 4 is generally used in a
ratio of A to B
of 1:10 to 10:1, preferably 1:2 to 4:1, with B being applied at a rate of 1 to
1000 g/ha,
20 preferably 20 to 500 g/ha. Combination 5 is generally used in a ratio of A
to B of 1:500 to
50:1, preferably 1:20 to 10:1, with B being applied at a rate of 10 to 1000
g/ha, preferably 50
to 500 g/ha. Combination 6 is generally used in a ratio of A to B 1 of 3:1 to
50:1, preferably
5:1 to 30:1, and a ratio of A to B2 of 1:10 to 10:1, preferably 1:2 to 2:1,
with B 1 being
applied at a rate of 1 to 100 g/ha, preferably 5 to 50 g/ha, and B2 being
applied at a rate of 10
25 to 1000 g/ha, preferably 50 to 500 g/ha. Combination 7 is generally used in
a ratio of A to
B3 of 2:1 to 20:1, preferably 4:1 to 10:1, and a ratio of A to B4 of 1:10 to
10:1, preferably
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1:2 to 2:1, with B3 being applied at a rate of 1 to 100 g/ha, preferably 20 to
70 glha, and B4
being applied at a rate of 10 to 1000 g/ha, preferably 50 to 500 g/ha.
b) Compound 131 (Index Table C, mixture partner A, generally applied at a rate
of 10
to 1000 g/ha, preferably applied at a rate of 50 to 500 g/ha) in combination
with:
Combination
Number Mixture partner B
1 rimsulfuron
2 nicosulfuron
3 dichlormid
4 benoxacor
naphthalic anhydride
6 rimsulfuron (B 1 ) in combination with dichlormid (B2)
7 nicosulfuron (B3) in combination with dichlormid (B4)
Combination 1 is generally used in a ratio of A to B of 3:1 to 50:1,
preferably 5:1 to
30:1, with B being applied at a rate of 1 to 100 g/ha, preferably 5 to 50
g/ha. Combination 2
is generally used in a ratio of A to B of 2:1 to 20:1, preferably 4:1 to 10:1,
with B being
applied at a rate of 1 to 100 g/ha, preferably 20 to 70 g/ha. Combination 3 is
generally used
in a ratio of A to B of 1:10 to 10:1, preferably 1:2 to 2:1, with B being
applied at a rate of 10
to 1000 g/ha, preferably 50 to 500 g/ha. Combination 4 is generally used in a
ratio of A to B
of 1:10 to 10:1, preferably 1:2 to 4: l, with B being applied at a rate of 1
to 1000 g/ha,
preferably 20 to 500 g/ha. Combination 5 is generally used in a ratio of A to
B of 1:500 to
50:1, preferably 1:20 to 10:1, with B being applied at a rate of 10 to 1000
g/ha, preferably 50
to 500 g/ha. Combination 6 is generally used in a ratio of A to B 1 of 3:1 to
50:1, preferably
S:1 to 30:1, and a ratio of A to B2 of 1:10 to 10:1, preferably 1:2 to 2:1,
with B 1 being
applied at a rate of 1 to 100 g/ha, preferably 5 to 50 g/ha, and B2 being
applied at a rate of 10
to 1000 g/ha, preferably 50 to 500 g/ha. Combination 7 is generally used in a
ratio of A to
B3 of 2:1 to 20:1, preferably 4:1 to 10:1, and a ratio of A to B4 of 1:10 to
10:1, preferably
1:2 to 2:1, with B3 being applied at a rate of 1 to 100 g/ha, preferably 20 to
70 g/ha, and B4
being applied at a rate of 10 to 1000 g/ha, preferably 50 to 500 g/ha.
c) Compound 242 (Index Table C, mixture partner A, generally applied at a rate
of 10
to 1000 g/ha, preferably applied at a rate of 50 to 500 g/ha) in combination
with:
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Combination
Number Mixture partner B
1 Rimsulfuron
2 Nicosulfuron
3 Dichlormid
4 Benoxacor
naphthalic anhydride
6 rimsulfuron (B 1 ) in combination with dichlormid (B2)-
7 nicosulfuron (B3) in combination with dichlormid (B4)
Combination 1 is generally used in a ratio of A to B of 3:1 to 50: l,
preferably 5:1 to
30:1, with B being applied at a rate of 1 to 100 g/ha, preferably 5 to 50
g/ha. Combination 2
S is generally used in a ratio of A to B of 2:1 to 20:1, preferably 4:1 to
10:1, with B being
applied at a rate of 1 to 100 g/ha, preferably 20 to 70 g/ha. Combination 3 is
generally used
in a ratio of A to B of 1:10 to 10:1, preferably 1:2 to 2:1, with B being
applied at a rate of 10
to 1000 g/ha, preferably 50 to 500 g/ha. Combination 4 is generally used in a
ratio of A to B
of 1:10 to 10:1, preferably 1:2 to 4: l, with B being applied at a rate of 1
to 1000 g/ha,
preferably 20 to S00 g/ha. Combination S is generally used in a ratio of A to
B of 1:500 to
50:1, preferably 1:20 to 10: l, with B being applied at a rate of 10 to 1000
g/ha, preferably 50
to S00 g/ha. Combination 6 is generally used in a ratio of A to B1 of 3:1 to
50:1, preferably
5:1 to 30: l, and a ratio of A to B2 of 1:10 to 10:1, preferably 1:2 to 2:1,
with B 1 being
applied at a rate of 1 to 100 g/ha, preferably 5 to 50 g/ha, and B2 being
applied at a rate of 10
to 1000 g/ha, preferably 50 to 500 g/ha. Combination 7 is generally used in a
ratio of A to
B3 of 2:1 to 20:1, preferably 4:1 to 10:1, and a ratio of A to B4 of 1:10 to
10:1, preferably
1:2 to 2: l, with B3 being applied at a rate of 1 to 100 g/ha, preferably 20
to 70 g/ha, and B4
being applied at a rate of 10 to 1000 g/ha, preferably 50 to 500 glha.
d) Compound 146 (Index Table C, mixture partner A, generally applied at a rate
of 10
to 1000 g/ha, preferably applied at a rate of 50 to 500 g/ha) in combination
with:
Combination
Number Mixture partner B
1 Rimsulfuron
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2 Nicosulfuron
3 Dichlormid
4 Benoxacor
naphthalic anhydride
6 rimsulfuron (B1) in combination with dichlorniid (B2)
7 nicosulfuron (B3) in combination with dichlormid (B4)
Combination 1 is generally used in a ratio of A to B of 3:1 to 50:1,
preferably 5:1 to
30:1, with B being applied at a rate of 1 to 100 g/ha, preferably 5 to 50
g/ha. Combination 2
is generally used in a ratio of A to B of 2:1 to 20:1, preferably 4:1 to 10:1,
with B being
5 applied at a rate of 1 to 100 g/ha, preferably 20 to 70 g/ha. Combination 3
is generally used
in a ratio of A to B of 1:10 to 10:1, preferably 1:2 to 2: l, with B being
applied at a rate of 10
to 1000 g/ha, preferably 50 to 500 g/ha. Combination 4 is generally used in a
ratio of A to B
of 1:10 to 10:1, preferably 1:2 to 4:1, with B being applied at a rate of 1 to
1000 g/ha,
preferably 20 to S00 g/ha. Combination 5 is generally used in a ratio of A to
B of 1:500 to
50:1, preferably 1:20 to 10:1, with B being applied at a rate of 10 to 1000
g/ha, preferably 50
to S00 g/ha. Combination 6 is generally used in a ratio of A to B 1 of 3:1 to
50:1, preferably
5:1 to 30:1, and a ratio of A to B2 of 1:10 to 10: l, preferably 1:2 to 2:1,
with B 1 being
applied at a rate of 1 to 100 g/ha, preferably 5 to 50 g/ha, and B2 being
applied at a rate of 10
to 1000 g/ha, preferably SO to 500 g/ha. Combination 7 is generally used in a
ratio of A to
B3 of 2:1 to 20:1, preferably 4:1 to 10:1, and a ratio of A to B4 of 1:10 to
10:1, preferably
1:2 to 2:1, with B3 being applied at a rate of 1 to 100 g/ha, preferably 20 to
70 g/ha, and B4
being applied at a rate of 10 to 1000 g/ha, preferably 50 to 500 g/ha.
The following Tests demonstrate the control efficacy of the compounds of this
invention against specific weeds. The weed control afforded by the compounds
is not
limited, however, to these species. See Index Tables A-D for compound
descriptions. The
abbreviation "dec" indicates that the compound appeared to decompose on
melting. The
abbreviation "Ex." stands for "Example" and is followed by a number indicating
in which
example the compound is prepared.
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INDEX TABLE A
R16 ~ ~ O O
\ ~ R1
N~
p R2
O
Cmpd RI R2 R16 rlp(~C)
No.
1 Et Et 4-OCH 113-116
2 Et Et 2,6-dimethyl 90-93
3 Et Et 4-F 71-76
4 i-Pr 4-F-Phenyl 2-CH 122-124
i-Pr 4-F-Phenyl 4-OCH 145-148
6 i-Pr 3, 6-dihydro-2H pyran4-OCH 98-100
7 (Ex.l)i-Pr 4-F-Phenyl 2,4-di-CI 57-60
8 i-Pr 4-F-Phenyl 2-C1 80-83
9 i-Pr 3, 6-dihydro-2H pyran3,5-di-C1 137-139
i-Pr 3, 6-dihydro-2H pyran2-CH 143-145
11 Et Et 3,5-di-Cl oil*
12 Et Et 4-OCF oil*
13 i-Pr 3, 6-dihydro-2H pyran4-OCF oil*
14 i-Pr 4-F-Phenyl 2-OCF 129-131
i-Pr 4-F-Phenyl 2-CF 131-134
16 i-Pr 4-F-Phenyl 2,5-di-C1 120-122
17 i-Pr 4-F-Phenyl 1, 4-di-Me 154-156
18 i-Pr 4-F-Phenyl 2,6-di-Me 103-105
19 i-Pr 4-F-Phenyl 2,6-di-CI 130-132
i-Pr 4-F-Phenyl 4-CI-2-CF 128-131
21 i-Pr 4-F-Phenyl 3-CI-2-Me 170-172
22 i-Pr 2,4-di-F-Phenyl 2,4-di-F 108-110
23 Et c-Hex 2,4-di-F oil*
24 i-Pr 2,4-di-F-Phenyl 2,4-di-Me 103-106
i-Pr 2,4-di-F-Phenyl 2-Me 85-89
26 Et c-Hex 2,4-di-Me 118-120
27 Et c-Hex 2,6-di-Me 120-122
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28 i-Pr 2,4-di-F-Phenyl 2,6-di-Me 129-131
29 Et c-Hex 2-OMe 111-114
30 i-Pr 4-F-Phenyl 2-OMe 109-111
31 i-Pr 2,4-di-F-Phenyl 2-OMe 55-60
32 i-Pr 2,4-di-F-Phenyl 2,4-di-OMe 134-137
33 i-Pr 4-F-Phenyl 2,4-di-OMe 175-177
34 i-Pr 4-F-Phenyl 2-Et 94-97
35 i-Pr 4-F-Phenyl 2-Me-4-OMe 112-115
36 i-Pr Phenyl 2-Me 148-150
37 c-Pr 4-F-Phenyl 2-Me oil*
38 i-Pr 4-F-Phenyl H oil*
39 i-Pr 4-CF -Phenyl 2-Me 85
40 i-Pr 4-Me-Phenyl 2-Me 128
41 i-Pr 4-Cl-Phenyl 2-Me 139-141
42 i-Pr 2,4-di-Cl-5-O-i-Pr-Phenyl2-Me 68-70
43 i-Pr 4-F-Phenyl 2,4-di-Cl-S-O-i-Pr148-150
44 i-Pr 4-NO -Phenyl 2-Me 148
45 i-Pr 2,4-di-F-Phenyl 2-Et 93-97
46 (Ex.2)i-Pr Phenyl 2,6-di-Me 146-148
47 i-Pr 4-CI-Phenyl 2,6-di-Me 143-147
48 i-Pr 3,4-di-F-Phenyl 2-Me 124
49 i-Pr 4-OMe-Phenyl 2-Me 95
50 c-Pr 2,4-diF-Phenyl 2-Me oil*
51 i-Pr 4-CN Phenyl 2-Me 205
52 i-Pr 4-F-Phenyl 2-Et-6-Me oil*
53 i-Pr 4-F-Phenyl 2-CI-6-Me oil*
54 i-Pr 4-Cl-Phenyl 2-Cl-6-Me oil*
55 i-Pr Pyrrolidinyl 2,4-di-CI 120-122
56 i-Pr Pyrrolidinyl 2-OCF oil*
57 i-Pr Pyrrolidinyl 2-CF 120-122
58 i-Pr Pycrolidinyl 2, 5-di-CI 139-140
59 i-Pr Pyrrolidinyl 2-Me 103-106
60 i-Pr 4-F-Phenyl 2,4, 6-tri-Me 181-183
61 i-Pr 4-Cl-Phenyl 2,4, 6-tri-Me 121-122
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86
62 i-Pr 4-F-Phenyl 2-Me-6-OMe 100-102
63 Et c-Hex 2,4, 6-tri-Me 122-123
64 i-Pr 4-Cl-Phenyl 2-i-Pr, 6-Me oil*
65 i-Pr 4-F-Phenyl 2-i-Pr, 6-Me oil*
66 i-Pr Phenyl 2-i-Pr, 6-Me oil*
67 i-Pr 3,5-di-F 2-Me 120
68 i-Pr 2, 5-di-F 2-Me 98
69 i-Pr Benryl 2,6-di-Me oil*
70 Et Benzyl 2,6-di-Me oil*
71 Et Benzyl 2-Me oil*
72 i-Pr Benzyl 2-Me oil*
73 i-Pr Phenyl 2-OMe, 6-Me 132-134
74 i-Pr 2,4-di-F-Phenyl 2-OMe, 6-Me 107-109
*see Index Table B for 1H NMR data.
INDEX TABLE B
Cmpd 1H NMR Data (CDCl3 solution unless indicated otherwise)a
No.
11 8 1.25 (t, 6H), 3.40 (m, 4H), 6.96 (s, 1H), 7.55
(s, 1H), 8.59 (s, 1H).
12 8 1.26 (t, 6H), 3.58 (m, 4H), 7.36 (d, 2H), 7.61
(d, 2H).
13 8 1.33 (d, 6H) 2.3-2.4 (m, 2H), 3.86 (t, 2H), 4.2-4.3
(m, 2H), 4.38-4.45 (m, 1H), 5.83-5.90
7.38 (m, 2H), 7.60 (m, 2H).
23 b 7.5-7.4 (m, 1H), 7.1 (t, 2H), 4.2-3.8 (m, 1H),
3.5-3.2 (m, 2H), 2.0-1.8 (m, 3H), 1.8-1.0
37 S 7.3-7.4 (m, 6H), 7.0-7.1 (t, 2H), 3.4 (m, 1H),
2.21 (s, 3H), 0.9 (m, 2H), 0.7-0.8 (m, 2H).
38 8 7.4-7.6 (m , 4H), 7.3 (m, 1H), 7.0-7.2 (m, 2H),
4.7 (m, 1H), 1.2 (d, 6H).
50 b 7.3-7.4 (m, 4H), 7.2 (d, 1H), 6.8-7.0 (q, 2H),
3.4 (m, 1H), 2.2 (s, 3H), 0.9 (d, 2H), 0.8 (d,
52 8 7.2-7.4 (m, 3H), 7.0-7.2 (m, 4H), 4.7 (m, 1H),
2.3-2.4 (q, 2H), 2.1 (s, 3H), 1.2 (d, 6H), 1.
(t, 3H).
53 S 7.3 (m, 3H), 7.2 (m, 2H), 7.1 (t, 2H), 4.6-4.7
(m, 1H), 2.19 (s, 3H), 1.2 (d, 6H).
54 8 7.3-7.4 (q, 4H), 7.2 ( m, 3H), 4.6-4.7 (m, 1H),
2.198 (s, 3H), 1.2 (d, 6H).
69 8 7.4-7.1 (m, 8H), 4.68 (s, 2H), 4.5 (bs, 1H), 2.23
(s, 6H), 1.27 (d, 6H).
70 8 7.4-7.1 (m, 8H), 4.74 (s, 2H), 3.6-3.4 (bs, 2H),
2.26 (s, 6H), 1.2 (m, 3H).
71 8 7.5-7.3 (m, 9H), 4.74 (m, 2H), 3.6-3.4 (bm, 2H),
2.30 (s, 3H), 1.2 (bt, 3H).
72 8 7.5-7.1 (m, 9H), 4.67 (s, 2H), 4.5 (bs, 1H), 2.27
(s, 3H), 1.28 (d, 6H).
a iH NMR data are in ppm downfield from tetramethylsilane. Couplings are
designated by (s)-singlet,
(d)-doublet, (t)-triplet, (q)-quartet, (m)-multiplet, (dd)-doublet of
doublets, (dt)-doublet of triplets,
(br s)-broad singlet.
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INDEX TABLE C
o o
R1
N~
p R2
O
Cmpd. Q Rl 1' R2 MP C
75 1,3,5-Trimethylpyrazol-4-yli-Pr 4-F-Phenyl 152-154
76 1,3,5-Trimethylpyrazol-4-yli-Pr 2,4-diF-Phenyl 45-50
77 2-Thienylmethyl Et Et oil*
78 (Ex.9)Benzyl f-Pr 4-F-Phenyl 95-96
79 Benzyl i-Pr 2,4-diF-Phenyl 93-95
80 2-Thienylmethyl i-Pr 4-F-Phenyl oil*
81 2-Thienylmethyl i-Pr 2-Dihydropyranyl oil*
82 2-Thienylmethyl Et c-Hexyl oil*
83 2-Thienylmethyl Me Phenyl oil*
84 2-Methylbenryl Et Et oil*
85 2-Methylbenzyl Me Ph oil*
86 2-Thienylmethyl i-Pr 2,4-diF-Ph 77-80
87 2-Methylbenryl i-Pr 2,4-diF-Phenyl oil*
88 2-Methylbenzyl i-Pr 4-F-Phenyl 118-120
89 5-TetrahydronaphthylEt Et oil*
90 5-Tetrahydronaphthyli-Pr 4-F-Phenyl oil*
91 n-Propyl i-Pr 4-F-Phenyl oil*
92 n-Propyl i-Pr Phenyl oil*
93 Allyl i-Pr Phenyl 68-70
94 Benzyl i-Pr Phenyl 90-94
95 1,3-Dimethyl-5-chloropyrazol-4i-Pr 4-F-Phenyl 109-112
yl
96 1,3-Dimethyl-5-chloropyrazol-4i-Pr 2,4-diF-Phenyl 55-59
yl
97 1-Methyl-5-chloropyrazol-4-yli-Pr 4-F-Phenyl 55-60
98 1-Methylpyrazol-4-yli-Pr 4-F-Phenyl 145-146
99 2-Trifluoromethylcyclohexyli-Pr 4-F-Phenyl oil*
100 3-Phenyl-5-methylisoxazol-4-yli-Pr 4-F-Phenyl 206-209
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101 3-Ethyl-5-methylisoxazol-4-yli-Pr 4-F-Phenyl oil*
102 3-Ethyl-5-ethylisoxazol-4-yli-Pr 4-F-Phenyl 74-77
103 2-Thienylmethyl i-Pr Phenyl 90-95
104 2-Methoxybenzyl i-Pr Phenyl 115-117
105 Allyl i-Pr 4-Cl-Phenyl oil*
106 Benzyl i-Pr 4-Cl-Phenyl oil*
107 Ethyl i-Pr 4-F-Phenyl 78-81
108 Ethyl i-Pr 4-C1-Phenyl 83-86
109 Isopropyl i-Pr 2,4-diF-Phenyl 82-85
110 c-Hexyl i-Pr 4-F-Phenyl 128-131
111 c-Hexyl i-Pr 4-Cl-Phenyl 126-130
112 c-Hexyl i-Pr Phenyl 136-139
113 (Ex.l4)Isopropyl i-Pr Phenyl 82-86
114 Isopropyl i-Pr 4-Cl-Phenyl 76-80
115 c-Hexyl i-Pr 2,4-diF-Phenyl 88-90
116 Ethyl i-Pr 2,4-diF-Phenyl 75-77
117 Ethyl i-Pr Phenyl 74-76
118 t Bu i-Pr 4-Cl-Phenyl 88-90
119 n-Pr i-Pr 4-Cl-Phenyl oil*
120 1,3,5-Trimethylpyrazol-4-yli-Pr Phenyl 48-52
121 1,3-Dimethyl-5-chloropyrazol-4i-Pr Phenyl 54-56
yl
122 1-Methyl-5-chloropyrazol-4-yli-Pr Phenyl 94-97
123 1-Methylpyrazol-4-yli-Pr Phenyl 111-112
124 1-Methylpyrazol-5-yli-Pr 4-F-Phenyl 52-59
125 1, 4-Dimethylpyrazol-5-yli-Pr 4-F-Phenyl 45-49
126 3,5-di-Me-isoxazol-4-yli-Pr 2-Dihydropyranyloil*
127 Allyl c-Pr 2,4-F-Phenyl oil*
128 CH2C0 Et i-Pr 4-F-Phenyl oil*
129 t-Bu i-Pr Phenyl oil*
130 n-Pr i-Pr 2,4-diF-Phenyl oil*
131 (Ex.l3)i-Pr i-Pr 4-F-Phenyl 78-80
132 i-Pr i-Pr 4-Me-Phenyl 68-71
133 a-Me-Benzyl i-Pr 4-Cl-Phenyl oil*
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134 a-Me-Benryl i-Pr 4-F-Phenyl oil*
135 3,5-Diisopropylisoxazol-4-yli-Pr 4-F-Phenyl oil*
136 (Ex.S)2-Methylbenzyl i-Pr 4-Cl-Phenyl oil*
137 (Ex.7)Methyl i-Pr 4-CI-Phenyl 121-123
138 (Ex.6)Methyl i-Pr 4-F-Phenyl 135-136
139 2-Methylallyl i-Pr 4-F-Phenyl oil*
140 2-Chlorobenzyl i-Pr 4-F-Phenyl oil*
141 2-Chlorobenzyl i-Pr Pyrrolidinyl oil*
142 2-Methoxybenzyl i-Pr Pyaolidinyl oil*
143 2-Methoxybenzyl i-Pr 4-F-Phenyl 104-106
144 2-Chlorobenzyl i-Pr 2-Dihydropyranyl oil*
145 2-Chlorobenzyl i-Pr c-Hexenyl oil*
146 (Ex.3)Allyl i-Pr 4-F-Phenyl 65-66
147 Allyl i-Pr 2-Dihydropyranyl oil*
148 2-Chloroethyl i-Pr 4-F-Phenyl oil*
149 2-Chloroethyl i-Pr 2-Dihydropyraayl oil*
150 Allyl Et Pyaolidinyl oil*
151 Allyl i-Pr 2,4-diF-Phenyl oil*
152 Benryl Et Et oil*
153 Benzyl Me Phenyl oil*
154 Allyl c-Pr 4-F-Phenyl oil*
155 3,5-Dimethylisoxazol-4-yli-Pr 4-F-Phenyl 133-136
156 3,5-Dimethylisoxazol-4-yli-Pr 2,4-diF-Phenyl 175-178
157 3,5-Dimethylisothiazol-4-yli-Pr 4-F-Phenyl oil*
158 3,5-Dimethylisothiazol-4-yli-Pr 2,4-di-F-Phenyl 158-161
159 3,5-Dimethylisothiazol-4-yli-Pr 4-Cl-Phenyl 124-127
160 2, 5-Dichlorothiazoly-4-yli-Pr 4-F-Phenyl oil*
161 2-Me-c-Hex i-Pr 4-F-Phenyl 78-81
162 2-Me-c-Hex i-Pr Phenyl oil*
163 CF CH i-Pr 4-F-Phenyl 122-124
164 H i-Pr 4-F-Phenyl 55-60
165 i-Pr i-Pr Benzyl oil*
166 i-Pr Et Benzyl oil*
167 a-Me-Benzyl (S) i-Pr 4-F-Phenyl oil*
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168 a-Me-Benzyl (S) i-Pr Phenyl oil*
169 (Ex.B)i-Bu i-Pr 4-F-Phenyl 80-81
170 (Ex.4)NMe2 i-Pr 4-F-Phenyl 69-71
171 2-Methylphenyl i-Pr 2, 3-DiF-Phenyl 88
172 2-Methyl-c-hexyl i-Pr 2,4-DiF-Phenyl oil*
173 a-Methylbenzyl (S) i-Pr Phenyl 72-74
174 a-Methylbenzyl (S) i-Pr 4-Cl-Phenyl oil*
175 2-Methylphenyl i-Pr 4-Br-Phenyl 117
176 2-Methylphenyl i-Pr 2,6-di-F-Phenyl 91
177 Phenyl (Me)N i-Pr 4-F-Phenyl 62-64
178 a-Methylbenryl (R) i-Pr 4-Cl-Phenyl oil*
179 a-Methylbenzyl (R) i-Pr 4-F-Phenyl 64-67
180 2,6-DiMe-Phenyl i-Pr 4, 6-Dimethoxy-1,3,5-oil*
Triazine-2-yl
181 2-Me-Phenyl i-Pr 4, 6-Dimethoxy-1,3,5-oil*
Triazine-2-yl
182 i-Propyl i-Pr 4, 6-Dimethoxy-1,3,5-oil*
Triazine-2-yl
183 Phenyl (Me)N Et c-Hexyl oil*
184 3-Trifluoromethylcyclohexyli-Pr 4-F-Phenyl oil*
185 2-Methylphenyl i-Pr 2,4-DiCI-Phenyl 54
186 2-Methylphenyl i-Pr 2-CI, 4-F-Phenyl 48-51
187 2-Methylphenyl i-Pr 4-Ph-Phenyl 63
188 Oxiranylmethyl i-Pr 4-F-Phenyl oil*
189 i-Propyl Et 4-Pyridylmethyl oil*
190 i-Propyl Et 1,3,4-Thiadiazol-2-yloil*
191 (2,4-Dimethylthiazol-5-i-Pr 4-Cl-Phenyl oil*
yl)methyl
192 (2,4-Dimethylthiazol-5-i-Pr 4-F-Phenyl oil*
yl)methyl
193 2-Methylphenyl 3-Pentyl 4-F-Phenyl 142-145
194 Allyl c-Bu 4-F-Phenyl 61-63
195 2-Methylphenyl i-Pr 4-CI, 2-F-Phenyl 50
196 2,4-Dimethylthiazol-5-yli-Pr 4-Cl-Phenyl oil*
197 2,4-Dimethylthiazol-S-yli-Pr Phenyl oil*
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198 2,4-Dimethylthiazol-5-yli-Pr 4-F-Phenyl oil*
199 1-(3-Methyl-3-Butenyl)i-Pr 4-F-Phenyl 77-78
200 2-Methylphenyl c-Bu 4-F-Phenyl 108-110
201 2-Et-6-Me-Phenyl i-Pr 4-F-Phenyl oil*
202 4-Trifluoromethoxyphenyli-Pr 4-F-Phenyl 88-92
203 2-Methylphenyl i-Pr 4-Methylsulfonylphenyl153
204 2-Methylphenyl i-Pr 2-F-Phenyl 42
205 2-Methylphenyl i-Pr 4-Methylthiophenyl104
206 2-Furanylmethyl i-Pr 4-Cl-Phenyl oil*
207 2-Furanylmethyl i-Pr 4-F-Phenyl oil*
208 2-Furanyhnethyl i-Pr 2,4-diF-Phenyl oil*
209 2-Furanylmethyl i-Pr Phenyl 67-70
210 Cinnamyl i-Pr 4-F-Phenyl oil*
211 4-Acetoxybutyl i-Pr 4-F-Phenyl 93-95
212 Propargyl i-Pr 4-F-Phenyl 74-75
213 3-Trimethylsilylpropargyli-Pr 4-F-Phenyl oil*
214 1-(3-Ethoxycarbonyl-2-i-Pr 4-F-Phenyl oil*
Propenyl)
215 MeO2CCH2 i-Pr 4-F-Phenyl oil*
216 t-BuCOCH2 i-Pr 4-F-Phenyl oil*
217 MeCOCH2 i-Pr 4-F-Phenyl oil*
218 1-(3,4,4-Trifluoro-3-Butenyl)i-Pr 4-F-Phenyl oil*
219 2-(1,3-Dioxolan-2-yl)ethyli-Pr 4-F-Phenyl 94-96
220 CH30CHzCH20CHz i-Pr 4-F-Phenyl oil*
221 n-Butyl i-Pr 4-F-Phenyl oil*
222 2,4-DiMe-6-OMe-Phenyli-Pr 4-F-Phenyl oil*
223 2,4-DiMe-6-OMe-Phenyli-Pr 2,4-diF-Phenyl oil*
224 2-Br-4, 6-diMe-Phenyli-Pr 4-F-Phenyl 141-144
225 MeiN i-Pr Phenyl oil*
226 3-Methyl-3-oxetanylmethyli-Pr 4-F-Phenyl 65-77
227 1-(3,3,3-Trifluoro-2-i-Pr 4-F-Phenyl 80-105
methoximino)propyl
228 Methyl Et c-Hex 65-74
229 2-Methylphenyl i-Pr 4-n-Bu-Phenyl oil*
230 2-Methylphenyl i-Pr 4-Et-Phenyl oil*
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231 2-Methylphenyl i-Pr 4-i-Pr-Phenyl f 94
232 (2,4-DiMe-Thiazol-5-yl)methyl i-Pr 4-F-Phenyl oil*
233 (2,4-DiMe-Thiazol-5-yl)methyl i-Pr 2,4-diF-Phenyl oil*
234 3-Pyridyl i-Pr 4-F-Phenyl 109-112
235 3-Pyridyl i-Pr Phenyl 116-118
236 2-Methylphenyl i-Pr 2-Me-Phenyl oil*
237 2-Methylphenyl i-Pr 4-Dimethylamino-Phenyl115
238 a-Me-Benzyl (R) i-Pr 2,4-diF-Phenyl oil*
239 2-Methylphenyl s-Bu 4-F-Phenyl 79-82
240 2-Methylphenyl 1-c-Pr-ethyl4-F-Phenyl 90-93
241 c-Propyl i-Pr 4-Cl-Phenyl oil*
242 c-Propyl i-Pr 4-F-Phenyl 65-67
243 c-Propyl i-Pr Phenyl 70-74
244 2,6-DiMe-Phenyl 1-Ethoxy 4-F-Phenyl 97-99
carbonylethyl
245 D3C i-Pr 4-F-Phenyl 141-143
246 Neopentyl i-Pr 4-F-Phenyl 106-108
247 2-Methylphenyl 1-Ethoxy 4-F-Phenyl 97-99
carbonylethyl
248 Ethyl 1-Ethoxy 4-F-Phenyl oil*
carbonylethyl
249 Allyl c-Heptyl 4-F-Phenyl 72-79
250 2-Phenethyl i-Pr 4-F-Phenyl 95-96
251 c-Propylmethyl i-Pr 4-F-Phenyl oil*
252 CH3CHZC(O)CHZ i-Pr 4-F-Phenyl oil*
253 n-C,~I39 i-Pr 4-F-Phenyl oil*
254 1-(2-Octynyl) i-Pr 4-F-Phenyl oil*
255 2-( 1,3-Dioxan-2-yl)ethyli-Pr 4-F-Phenyl 82-83
256 1-(2-Trimethylsilylmethyl-2-i-Pr 4-F-Phenyl oil*
P~P~YI)
257 2-Cyclohexylethyl i-Pr 4-F-Phenyl oil*
258 CH30CHZCHZOCH2 i-Pr 4-F-Phenyl 119-120
259 (3,5-dimethylisoxazol-4-i-Pr 4-F-Phenyl oil*
yl)methyl
260 PhC(O)CH(Me) i-Pr 4-F-Phenyl oil*
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261 PhCH20CH2 i-Pr 4-F-Phenyl 110-112
262 Geranyl i-Pr 4-F-Phenyl oil*
263 1-(3-Methoxycarbonyl-2-i-Pr 4-F-Phenyl oil*
Propenyl)
264 Et2NC(O)CHZ i-Pr 4-F-Phenyl oil*
265 t-BuOZCCH2 i-Pr 4-F-Phenyl oil*
266 MeOZCCHzCHZCH2 i-Pr 4-F-Phenyl oil*
267 2-Pyridylmethyl i-Pr 4-F-Phenyl oil*
268 2-Methylphenyl i-Pr 4-Phenoxy-Phenyl51
269 2-Methylphenyl i-Pr 3-F-Phenyl 128
270 2-Methylphenyl i-Pr 4-t-Bu-Phenyl oil*
271 c-Pentyl i-Pr 4-F-Phenyl 79-80
272 3-Thienyl i-Pr 4-F-Phenyl 125-128
273 2,6-DiMe-Phenyl i-Pr 2-Cyclohexenyl 105-112
274 Me2N Et c-Hex oil*
275 Neopentyl Et c-Hex oil*
276 Neopentyl i-Pr Phenyl 116-118
277 Neopentyl i-Pr 2,4-DiF-Phenyl oil*
278 2-Methylphenyl i-Pr 5-Indanyl 115
279 Allyl 1-Ethoxy 4-F-Phenyl oil*
carbonylethyl
280 c-Hexyl 1-Ethoxy 4-F-Phenyl oil*
carbonylethyl
281 2,3-Dihydro-2-Me-benzofuran-i-Pr 4-F-Phenyl 148-150
7-yl
282 c-Pentyl i-Pr 4-Cl-Phenyl 104-106
283 c-Pentyl i-Pr Phenyl oil*
284 c-Pentyl i-Pr 2,4-DiF-Phenyl oil*
285 1-(3-Chlorobutenyl)i-Pr 4-F-Phenyl oil*
286 1-(2-Pentenyl) i-Pr 4-F-Phenyl oil*
287 3-Fluoropropyl i-Pr 4-F-Phenyl oil*
288 1-(3-Methyl-2-butenyl)i-Pr 4-F-Phenyl oil*
289 1-(4-Fluorobutyl) i-Pr 4-F-Phenyl oil*
290 n-Pentyl i-Pr 4-F-Phenyl oil*
291 1-(4-Pentenyl) i-Pr 4-F-Phenyl oil*
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292 Acetoxymethyl i-Pr 4-F-Phenyl oil*
293 (Ex.lS)Methoxymethyl i-Pr 4-F-Phenyl oil*
294 Trimethylsilylmethyli-Pr 4-F-Phenyl oil*
295 Ethoxymethyl i-Pr 4-F-Phenyl oil*
296 i-Propyl i-Pr 2-Pyrazinyl oil*
297 c-Propyl Et Et oil*
298 c-Propyl Et c-Hex oil*
299 c-Propyl i-Pr 2,4-DiF-Phenyl 83-85
300 2-Methylphenyl i-Pr 4-CF30-Phenyl 109
301 2-Methylphenyl i-Pr 4-Pyridinyl 152-154
302 i-Propyl 1-Ethoxy 4-F-Phenyl oil*
carbonylethyl
303 2-t-Bu-6-Me-Phenyl i-Pr Phenyl oil*
304 2,6-DiEt-Phenyl i-Pr 4-F-Phenyl oil*
305 2,6-DiEt-Phenyl i-Pr Phenyl 77-83
306 2-Methylphenyl i-Pr 2-Naphthyl 49
307 Allyl Et c-Hex 62-65
308 c-Hexyl Et c-Hex oil*
309 i-Propyl Et c-Hex oil*
310 4-Tetrahydropyranyli-Pr 4-F-Phenyl 101-103
311 2-Tetrahydropyranyli-Pr 4-F-Phenyl 103-105
312 2-Furanylmethyl Et c-Hex oil*
313 2-Hiphenylylmethyl i-Pr 4-F-Phenyl 113-126
314 1-(2-Methylthioethyl)i-Pr 4-F-Phenyl 101-106
315 2,6-DiMe-Phenyl i-Pr 2-Dihydropyranyl 122-124
316 2-(3-Methylbutyl) i-Pr 4-F-Phenyl 62-64
317 1-(2,2-Dimethoxyethyl)i-Pr 4-F-Phenyl oil*
318 2,6-DiMe-Phenyl c-Bu 2,4-DiCI-Phenyl 127-131
319 i-Propyl c-Bu 2,4-DiCI-Phenyl 103-106
320 (5-Cl-1,2,3-thiadiazol-4-i-Pr 2,4-DiF-Phenyl 103-108
yl)methyl
321 (5-Cl-1,2,3-thiadiazol-4-i-Pr Phenyl 128-131
yl)methyl
322 Cyclopentylmethyl i-Pr 4-F-Phenyl 83-90
323 1-(3-Dimethylaminopropyl)i-Pr 4-F-Phenyl oil*
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324 2-Methylphenyl 2-(3-OMe-propyl)4-F-Phenyl 115-121
325 Allyl 1-c-Pr-ethyl4-Cl-Phenyl oil*
326 [2.2.1]-Bicyclohept-2-yli-Pr 2,4-DiF-Phenyl 103-105
327 [2.2.1]-Bicyclohept-2-yli-Pr 4-F-Phenyl 90-94
328 [2.2.1]-Bicyclohept-2-yli-Pr Phenyl 90-91
329 2-Naphthyl i-Pr 4-F-Phenyl 150-151
330 2-Methylphenyl 1-c-Pr-ethyl4-Cl-Phenyl 111-115
331 2-Me0-6-Me-Phenyl 1-Ethoxy 4-F-Phenyl oil*
carbonylethyl
332 2-Naphthyl i-Pr Phenyl 134-135
333 2-Naphthyl i-Pr 4-Cl-Phenyl 142-143
334 2-Naphthyl i-Pr 4-Me-Phenyl 172-173
335 2-Naphthyl i-Pr 2,4-DiF-Phenyl oil*
336 1-Me-2-Naphthyl i-Pr 4-Cl-Phenyl oil*
337 1-Me-2-Naphthyl i-Pr 2,4-DiF-Phenyl oil*
338 1-Me-2-Naphthyl i-Pr 4-F-Phenyl oil*
339 c-Heptyl i-Pr 4-Cl-Phenyl 125-135
340 c-Heptyl i-Pr 4-F-Phenyl 104-105
341 c-Heptyl i-Pr Phenyl 100-102
342 c-Heptyl i-Pr 2,4-DiF-Phenyl 87-90
343 2-Tetrahydrofuranylmethyli-Pr 4-F-Phenyl 95-96
344 1-Me-2-Naphthyl i-Pr Phenyl oil*
345 2-Tetrahydrofuranyli-Pr 4-F-Phenyl oil*
346 (3,5-Dimethylpyrazol-1-i-Pr Phenyl 138-148
yl)methyl
347 (3,5-Dimethylpyrazol-1-i-Pr 4-F-Phenyl 140-144
yl)methyl
348 c-Butyl i-Pr Phenyl 70-72
349 c-Butyl i-Pr 4-Cl-Phenyl 64-68
350 c-Butyl i-Pr 4-F-Phenyl 97-100
351 c-Butyl i-Pr 2,4-diF-Phenyl 65-67
352 MeOCH2CH(Me) i-Pr 2,4-diF-Phenyl oil*
353 3-Pentyl i-Pr 2,4-diF-Phenyl 72-75
354 3-Pentyl i-Pr Phenyl oil*
355 2-(3-Methylbutyl) i-Pr Phenyl oil*
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356 2-(3-Methylbutyl) i-Pr 2,4-diF-Phenyl oil*
357 MeOCH2CH(Me) i-Pr 2,4-diF-Phenyl 81-85
358 3-Pentyl i-Pr 4-F-Phenyl oil*
359 2-t-Bu-6-Me-Phenyli-Pr 4-F-Phenyl oil*
360 1-(1-Me-c-propyl) i-Pr Phenyl 82-83
361 1-(1-Me-c-propyl) i-Pr 4-Cl-Phenyl oil*
362 I-(1-Me-c-propyl) i-Pr 4-F-Phenyl oil*
363 1-(1-Me-c-propyl) i-Pr 2,4-diF-Phenyl oil*
364 2-Methylphenyl Et Et oil*
365 Methyl 1-Ethoxy 4-F-Phenyl oil*
carbonylethyl
366 3-Pyridylmethyl i-Pr 4-F-Phenyl oil*
367 2-(3-Chloropropyl)i-Pr 4-F-Phenyl oil*
368 Methyl i-Pr 2,4-diF-Phenyl oil*
369 1-(2-Me-c-propyl) i-Pr 4-Cl-Phenyl oil*
370 1-(2-Me-c-propyl) i-Pr Phenyl oil*
371 1-(2-Me-c-propyl) i-Pr 4-F-Phenyl 95-97
372 1-(2-Me-c-propyl) i-Pr 2,4-diF-Phenyl oil*
373 (5-CI-3-Me-isothiazol-4-i-Pr 4-F-Phenyl 126-129
yl)methyl
374 (S-CI-3-Me-isothiazol-4-i-Pr Phenyl 133-136
yl)methyl
375 3-Tetrahydrofuryhnethyli-Pr 4-F-Phenyl 84-86
376 Chloromethyl i-Pr 4-F-Phenyl 83-86
377 H i-Pr 4-CI-Phenyl 137-138
378 (4-Methyl-1,2,3-thiadiazol-S-i-Pr Phenyl 109-113
yl)methyl
379 (2-Ethoxy-4-CF3-thiazol-5-i-Pr Phenyl oil*
yl)methyl
380 (4-Methyl-1,2,3-thiadiazol-5-i-Pr 4-F-Phenyl 54-55
yl)methyl
381 (2-Ethoxy-4-CF3-thiazol-S-i-Pr 4-F-Phenyl oil*
yl)methyl
382 I-(2,6-Dimethylpiperidine)i-Pr 4-F-Phenyl 97-100
383 1-(2,6-Dimethylpiperidine)i-Pr 2,4-diF-Phenyl 81-84
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384 4-(Morpholino) i-Pr 2,4-diF-Phenyl 62-68
385 4-(Morpholino) i-Pr 4-F-Phenyl 173-175
386 H i-Pr Phenyl 116-117
387 2-(2-Cyanoethyl) i-Pr 4-F-Phenyl oil*
388 1-(2-Cyanoethyl) i-Pr 4-F-Phenyl 125-128
389 n-Hexyl i-Pr 4-F-Phenyl oil*
390 2-(1,3-Difluoropropyl)i-Pr 4-F-Phenyl 99-101
391 H i-Pr 2,4-diF-Phenyl 110-112
392 Trans-1-(2-Me-c-propyl)i-Pr 4-F-Phenyl 90-91
393 1-(1-Chloroethyl) i-Pr 4-F-Phenyl 70-73
394 i-Butyl i-Pr 2,4-diF-Phenyl oil*
395 Cyanomethyl i-Pr 4-F-Phenyl 120-123
396 1-(2-Ethoxy-3-ethoxycarbonyl-i-Pr 4-F-Phenyl 112-114
2-propenyl)
397 1-(3,3,3-trifluoropropyl)i-Pr 4-F-Phenyl 99-100
398 1-(4,4,4-trifluorobutyl)i-Pr 4-F-Phenyl 71-72
399 1-(3,4,4, 4-Tetrafluoro-3-i-Pr 4-F-Phenyl oil*
trifluoromethylbutyl)
400 CH3C(O)CH(CH3) i-Pr 4-F-Phenyl oil*
401 1-(2-Cl-4-Me-thiazol-5-yl)ethyli-Pr 4-F-Phenyl oil*
402 2-Methyl-c-propylmethyli-Pr 4-F-Phenyl 81-83
403 c-Butylmethyl i-Pr 4-F-Phenyl 74-76
404 1-(c-Propylethyl) i-Pr 4-F-Phenyl 97-99
405 1-(2-Cl-4-Me-thiazol-5-yl)ethyli-Pr 2,4-diF-Phenyl 122-125
406 1-(2-CI-4-Me-thiazol-5-yl)ethyli-Pr 4-Cl-Phenyl 128-131
407 1-(2-Cl-4-Me-thiazol-S-yl)ethyli-Pr Phenyl 128-131
408 2-(3-Chloropropyl) i-Pr 2,4-diF-Phenyl oil*
409 Methyl i-Pr Phenyl 105-114
410 i-Butyl i-Pr Phenyl 55-67
411 2-(3-Chloropropyl) i-Pr Phenyl 95-105
412 1-(2-Butenyl) i-Pr 4-F-Phenyl oil*
413 2-(3-Butenyl) i-Pr 4-F-Phenyl oil*
414 Allyldimethylsilylmethyli-Pr 4-Cl-Phenyl oil*
415 1-(2-Bromoethyl) i-Pr Phenyl 90-92
416 4-Tetrahydropyranyli-Pr Phenyl 80-93
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417 i-Butyl i-Pr 4-Cl-Phenyl oil*
418 1-(3-Methyl-3-Butenyl)i-Pr Phenyl oil*
419 1-(2-Methylthioethyl)i-Pr Phenyl oil*
420 (3-Methyl-3-oxetanyl)methyli-Pr Phenyl oil*
421 2-(1,3-dilluoropropyl)i-Pr Phenyl 95-107
422 Chloromethyl i-Pr 4-Cl-Phenyl 75-77
423 Chloromethyl i-Pr Phenyl 75-77
424 Phenyldimethylsilylmethyli-Pr 4-Cl-Phenyl oil*
425 Vinyldimethylsilylmethyli-Pr 4-Cl-Phenyl oil*
426 Allyldimethylsilylmethyli-Pr 4-F-Phenyl oil*
427 c-Heptyl i-Pr 3, 6-dihydro-2H-pyranoil*
428 c-Heptyl i-Pr 1-Cyclohexenyl oil*
429 c-Heptyl Et c-Hexyl oil*
430 (5,6-Dihydro-1,2-Oxazin-3-i-Pr Phenyl 95-97
yl)methyl
431 Cyanomethyl i-Pr 2,4-diF-Phenyl 123-126
432 1-(1-Cyanoethyl) i-Pr 2,4-diF-Phenyl oil*
433 1-(2-Cyanoethyl) i-Pr 2,4-diF-Phenyl 112-114
434 Cyanomethyl i-Pr Phenyl 90-91
435 1-( 1-Cyanoethyl) i-Pr Phenyl oil*
436 1-(2-Cyanoethyl) i-Pr Phenyl 74-77
437 Chloromethyl i-Pr 2,4-diF-Phenyl 69-71
438 1-( 1-Chloroethyl)i-Pr Phenyl 73-75
439 1-(1-Methoxyethyl)i-Pr 4-F-Phenyl 77-79
440 MeZNC(O)CHz i-Pr 2,4-diF-Phenyl 111
441 1-( 1-Methoxyethyl)i-Pr Phenyl oil*
442 1-(2,4-Dimethylthiazol-5-i-Pr Phenyl oil*
yl)ethyl
443 1-(2,4-Dimethylthiazol-5-i-Pr 2,4-diF-Phenyl oil*
yl~thyl
444 1-(2-Cyanoethyl) i-Pr 4-Cl-Phenyl 139-142
445 PhCONHCH2 i-Pr 4-F-Phenyl 161-163
446 1-(1,2-Dimethoxyethyl)i-Pr 4-F-Phenyl oil*
447 (Et0)ZP(O)CHZ i-Pr Phenyl oil*
448 (Et0)ZP(O)CH(CH3) i-Pr Phenyl oil*
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449 1-(2-Ethyl-4-methylthiazol-5-i-Pr 4-F-Phenyl 106-109
yl)ethyl
450 (5,6-Dihydro-1,2-Oxazin-3-i-Pr 4-Cl-Phenyl 105-108
yl)methyl
451 1-(1-Cyanoethyl) i-Pr 4-Cl-Phenyl 117-127
452 1-(1-Methoxy-2-propenyl)i-Pr 4-F-Phenyl oil*
453 1-(2-Methylsulfonylethyl)i-Pr 4-F-Phenyl oil*
454 1-(2-Pentenyl) i-Pr Phenyl oil*
455 3-(4-Pentenyl) i-Pr Phenyl oil*
456 2-(3-Chloropropyl)i-Pr 4-Cl-Phenyl oil*
457 Hydroxymethyl i-Pr 4-Cl-Phenyl oil*
458 1-(2-Chloro-1-methoxyethyl)i-Pr 4-Cl-Phenyl oil*
459 Ethyldimethylsilylmethyli-Pr 4-F-Phenyl 54-55
460 Ethyldimethylsilylmethyli-Pr 4-Cl-Phenyl 68-71
461 1-(3-Trimethylsilylpropyl)i-Pr 4-F-Phenyl oil*
462 t-BuC(O)OCHZ i-Pr 4-F-Phenyl 87-90
463 CH30zCCH(CH3) i-Pr 2,4-diF-Phenyl oil*
464 CH302CCH(CH3) i-Pr Phenyl oil*
465 EtO2CCHzCH(COZEt) i-Pr 2,4-diF-Phenyl oil*
466 (3,4-Dihydroisoxazol-3-i-Pr 4-F-Phenyl 93-95
yl)methyl
467 Me3SiCH2CH20CH2 i-Pr 4-Cl-Phenyl oil*
468 2-(1,3-Difluoropropyl)i-Pr 4-Cl-Phenyl 93-96
469 1-(2-Chloroethyl) i-Pr Phenyl 80-83
470 Hydroxymethyl i-Pr 4-F-Phenyl 89-95
471 2-(3, 3-Dimethoxypropyl)i-Pr 4-F-Phenyl 60-63
472 2-(3, 3-Dimethoxypropyl)i-Pr 2,4-diF-Phenyl oil*
473 MeCONHCH2 i-Pr 4-F-Phenyl 150-168
474 1-(2-Chloroethyl) i-Pr 4-Cl-Phenyl 100-101
475 1-(2-Chloroethyl) i-Pr 2,4-diF-Phenyl 70-72
476 Cyanomethyl i-Pr 4-Cl-Phenyl 173-179
477 Me2NC(O)CHZ i-Pr 4-Cl-Phenyl 152-153
478 Me2NC(O)CH(CH3) i-Pr 4-F-Phenyl oil*
479 Me2NC(O)CH(CH3) i-Pr Phenyl oil*
480 Me2NC(O)CH(CH3) i-Pr 4-Cl-Phenyl 102
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481 MeZNC(O)CH(CH3) i-Pr 2,4-diF-Phenyl oil*
482 (2-Chlorothiazol-5-yl)methyli-Pr 4-F-Phenyl 69-70
483 1-(2-nitroethyl) i-Pr 4-Cl-Phenyl 119-122
484 i-PrC(CO)CHZ i-Pr 4-F-Phenyl 79-81
485 i-PrC(CO)CHZ i-Pr Phenyl oil*
486 i-PrC(CO)CHZ i-Pr 2,4-diF-Phenyl oil*
487 i-PrC(CO)CHZ i-Pr 4-Cl-Phenyl oil*
488 c-PrC(CO)CHZ i-Pr 4-F-Phenyl oil*
489 c-PrC(CO)CHZ i-Pr Phenyl 87-89
490 c-PrC(CO)CHZ i-Pr 2,4-diF-Phenyl oil*
491 HC(O)CHZ i-Pr 4-F-Phenyl oil*
492 CICHzC(O)NHCHZCHZ i-Pr Phenyl oil*
493 C1CHZC(O)NHCHZCHZCHZi-Pr Phenyl oil*
494 (5,6-Dihydro-1,3-oxazin-2-i-Pr Phenyl oil*
yl)methyl
495 (3,4-Dihydrooxazol-2-i-Pr Phenyl oil*
yl)methyl
496 (1-Cyclohexenyl)methyli-Pr Phenyl oil*
497 (1-Methyl-1,2,5,6-i-Pr Phenyl oil*
tetrahydropyridin-3-yl)methyl
498 1-(2-(3-Pyridyl)-2-propenyl)i-Pr Phenyl oil*
499 I-(2-Ethyl-4-methylthiazol-5-i-Pr 4-Cl-Phenyl 103-104
yl)ethyl
500 1-(3-Fluoropropyl)i-Pr 2,4-diF-Phenyl oil*
501 2-(1,3-Dioxolan-2-yl)ethyli-Pr 2,4-diF-Phenyl oil*
502 2-(1,3-Dioxan-2-yl)ethyli-Pr 2,4-diF-Phenyl oil*
503 Methoxymethyl i-Pr 2,4-diF-Phenyl oil*
504 Ethoxymethyl i-Pr 2,4-diF-Phenyl oil*
505 CH30CHZCHZOCH2 i-Pr 2,4-diF-Phenyl oil*
506 1-(4-Acetoxybutyl)i-Pr 2,4-diF-Phenyl oil*
507 1-(3,4,4-Trifluoro-3-butenyl)i-Pr 2,4-diF-Phenyl oil*
508 I-(2-Phenylethyl) i-Pr 2,4-diF-Phenyl oil*
509 Cyclopropylmethyl i-Pr 2,4-diF-Phenyl oil*
510 (3,5-Dimethyloxazol-4-i-Pr 2,4-diF-Phenyl oil*
yl)methyl
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S 11 PhCOCH(CH3) i-Pr 2,4-diF-Phenyl oil*
S 12 Et2NC(O)CHZ i-Pr 2,4-diF-Phenyl oil*
S 13 MeO2CCH2CH2CHz i-Pr 2,4-diF-Phenyl oil*
S 14 1-(3-Chloro-2-butenyl)i-Pr 2,4-diF-Phenyl oil*
S1S I-(3-Methyl-2-butenyl)i-Pr 2,4-diF-Phenyl oil*
S 16 1-(4-Pentenyl) i-Pr 2,4-diF-Phenyl oil*
S 17 CH3C(O)CH(CH3) i-Pr 2,4-diF-Phenyl oil*
S 18 Trimethylsilylmethyli-Pr 2,4-diF-Phenyl oil*
S 19 1-(2-Ethoxy-3-ethoxycarbonyl-i-Pr 2,4-diF-Phenyl oil*
2-propenyl)
S20 PhCHzOCHz i-Pr 2,4-diF-Phenyl oil*
S21 Cyclobutylmethyl i-Pr 2,4-diF-Phenyl oil*
522 I-(4-Fluorobutyl) i-Pr 2,4-diF-Phenyl oil*
S23 1-(2-Pentenyl) i-Pr 2,4-diF-Phenyl oil*
S24 CH3CHZC(O)CHZ i-Pr 2,4-diF-Phenyl oil*
S2S 1-(3,3,3-Trifluoropropyl)i-Pr 2,4-diF-Phenyl oil*
S26 1-(4,4,4-Trifluorobutyl)i-Pr 2,4-diF-Phenyl oil*
S27 n-Butyl i-Pr 4-Cl-Phenyl oil*
S28 n-Pentyl i-Pr 4-Cl-Phenyl oil*
S29 n-Hexyl i-Pr 4-CI-Phenyl oil*
S30 I-(3-Fluoropropyl)i-Pr 4-Cl-Phenyl oil*
S31 2-(1,3-Dioxolan-2-yl)ethyli-Pr 4-CI-Phenyl oil*
S32 2-(1,3-Dioxan-2-yl)ethyli-Pr 4-CI-Phenyl oil*
S33 Methoxymethyl i-Pr 4-Cl-Phenyl oil*
S34 Ethoxymethyl i-Pr 4-CI-Phenyl oil*
S3S CH30CHzCH20CH2 i-Pr 4-Cl-Phenyl oil*
S36 1-(4-Acetoxybutyl)i-Pr 4-Cl-Phenyl oil*
S37 1-(3,4,4-Trifluoro-3-butenyl)i-Pr 4-CI-Phenyl oil*
S38 I-(2-Phenylethyl) i-Pr 4-CI-Phenyl oil*
S39 Cyclopropylmethyl i-Pr 4-Cl-Phenyl oil*
S40 (3,S-Dimethyloxazol-4-i-Pr 4-CI-Phenyl oil*
yl)methyl
S41 PhCOCH(CH3) i-Pr 4-Cl-Phenyl oil*
S42 Et2NC(O)CHZ i-Pr 4-Cl-Phenyl oil*
S43 MeO2CCHZCH2CHz i-Pr 4-CI-Phenyl oil*
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544 1-(3-Chloro-2-butenyl)i-Pr 4-C1-Phenyl oil*
545 1-(3-Methyl-2-butenyl)i-Pr 4-Cl-Phenyl oil*
546 1-(4-Pentenyl) i-Pr 4-Cl-Phenyl oil*
547 CH3C(O)CH(CH3) i-Pr 4-Cl-Phenyl oil*
548 Trimethylsilylmethyli-Pr 4-Cl-Phenyl oil*
549 1-(2-Ethoxy-3-ethoxycarbonyl-i-Pr 4-Cl-Phenyl oil*
2-propenyl)
550 Cyclobutylmethyl i-Pr 4-Cl-Phenyl oil*
551 1-(4-Fluorobutyl) i-Pr 4-Cl-Phenyl oil*
552 1-(2-Pentenyl) i-Pr 4-Cl-Phenyl oil*
553 CH3CHZC(O)CHZ i-Pr 4-Cl-Phenyl oil*
554 1-(3,3,3-Trifluoropropyl)i-Pr 4-Cl-Phenyl oil*
555 1-(4,4,4-Trifluorobutyl)i-Pr 4-Cl-Phenyl oil*
556 n-Butyl i-Pr Phenyl oil*
557 n-Pentyl i-Pr Phenyl oil*
558 n-Hexyl i-Pr Phenyl oil*
559 1-(3-Fluoropropyl) i-Pr Phenyl oil*
560 2-(1,3-Dioxolan-2-yl)ethyli-Pr Phenyl oil*
561 2-(1,3-Dioxan-2-yl)ethyli-Pr Phenyl oil*
562 Methoxymethyl i-Pr Phenyl oil*
563 Ethoxymethyl i-Pr Phenyl oil*
564 CH30CHZCHZOCHz i-Pr Phenyl oil*
565 1-(4-Acetoxybutyl) i-Pr Phenyl oil*
566 1-(3,4,4-Trifluoro-3-butenyl)i-Pr Phenyl oil*
567 1-(2-Phenylethyl) i-Pr Phenyl oil*
568 Cyclopropyhnethyl i-Pr Phenyl oil*
569 (3,5-Dimethyloxazol-4-i-Pr Phenyl oil*
yl)methyl
570 PhCOCH(CH3) i-Pr Phenyl oil*
571 EtZNC(O)CHZ i-Pr Phenyl oil*
572 MeOzCCH2CH2CH2 i-Pr Phenyl oil*
573 1-(3-Chloro-2-butenyl)i-Pr Phenyl oil*
574 1-(3-Methyl-2-butenyl)i-Pr Phenyl oil*
575 i-(4-Pentenyl) i-Pr Phenyl oil*
576 CH3C(O)CH(CH3) i-Pr Phenyl oil*
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577 Trimethylsilylmethyli-Pr Phenyl oil*
578 1-(2-Ethoxy-3-ethoxycarbonyl-i-Pr Phenyl oil*
2-propenyl)
579 PhCHZOCH2 i-Pr Phenyl oil*
580 Cyclobutylmethyl i-Pr Phenyl oil*
581 1-(4-Fluorobutyl) i-Pr Phenyl oil*
582 1-(2-Pentenyl) i-Pr Phenyl oil*
583 CH3CHzC(O)CHZ i-Pr Phenyl oil*
584 1-(3,3,3-Trifluoropropyl)i-Pr Phenyl oil*
585 1-(4,4,4-Trifluorobutyl)i-Pr Phenyl oil*
586 MeZNC(O)CHZ i-Pr 4-F-Phenyl 117
587 (Et0)ZP(O)CHZ i-Pr 4-F-Phenyl oil*
588 Me2NC(O)CHZ i-Pr Phenyl 152
589 1-(2-Ethyl-4-methylthiazol-5-i-Pr 2,4-diF-Phenyl 87-90
yl)ethyl
590 1-(2-Ethyl-4-methylthiazol-5-i-Pr 4-Cl-Phenyl 93-97
yl)ethyl
591 1-(2-Nitroethyl) i-Pr 2,4-diF-Phenyl 92-98
592 1-(1-Methoxyethyl) i-Pr 4-Cl-Phenyl oil*
593 1-(1-Methoxyethyl) i-Pr 2,4-diF-Phenyl oil*
594 2-(3-Bromopropyl) i-Pr 2,4-diF-Phenyl oil*
595 2-(1,3-Difluoropropyl)i-Pr 2,4-diF-Phenyl 91-96
596 2-(3-Acetoxy-1-chloropropyl)i-Pr 4-F-Phenyl oil*
597 F3CC(O)CHZ i-Pr 4-Cl-Phenyl oil*
598 F3CC(O)CHZ i-Pr 2,4-diF-Phenyl oil*
599 (Et0)2P(O)CHZ i-Pr 4-Cl-Phenyl oil*
600 Allyl 2-(3-OMe-propyl)2,6-DiMe-Phenyl oil*
601 (5,6-Dihydro-1,2-Oxazin-3-i-Pr 4-F-Phenyl 108-112
yl)methyl
602 (5,6-Dihydro-1,2-Oxazin-3-i-Pr 2,4-diF-Phenyl 87-95
yl)methyl
603 1-(2-Nitropropyl) i-Pr 2,4-diF-Phenyl oil*
604 1-(2-Nitropropyl) i-Pr Phenyl oil*
605 1-(2-(6-Chloro-2-pyridyl)-2-i-Pr Phenyl oil*
propenyl)
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606 1-(2-(4-Fluorophenyl)-2-i-Pr Phenyl oil*
propenyl)
607 1-(2-Methyl-2-propenyl)i-Pr Phenyl oil*
608 1-(2-Chlorol-2-propenyl)i-Pr Phenyl oil*
609 2-(3-Butynyl) i-Pr Phenyl oil*
610 s-Butyl (R) i-Pr Phenyl 53-55
611 s-Butyl (S) i-Pr Phenyl 55-57
612 s-Butyl (S) i-Pr Phenyl 41-43
613 s-Butyl (R) i-Pr 4-F-Phenyl 41-43
614 EtOZCCHzCH(COZEt) i-Pr Phenyl oil*
615 EtO2CCH2CH(COZEt) i-Pr 4-F-Phenyl oil*
616 MeO2CCH(CH3) i-Pr 4-F-Phenyl oil*
617 (Et0)ZP(O)CH(CH3) i-Pr 4-F-Phenyl oil*
618 Thiocyanatomethyl i-Pr 4-F-Phenyl 125-127
~
619 PhC(O)NHCHZ i-Pr 2,4-diF-Phenyl 120-123
620 PhC(O)NHCHZ i-Pr Phenyl 145-146
621 MeC(O)NHCHZ i-Pr Phenyl 122-126
622 MeC(O)NHCHZ i-Pr 2,4-diF-Phenyl 173-175
623 MeO2CCH(CH3) i-Pr 4-CI-Phenyl oil*
624 (2-Tetrahydropyranyl)methyli-Pr 4-F-Phenyl 80-82
625 CH3C(O)N(CH3)CHZCHZi-Pr 4-F-Phenyl 112-126
626 1-(2-Fluoroethyl) i-Pr 4-F-Phenyl 95-96
627 1-(2-Methoxyethyl)i-Pr 4-F-Phenyl oil*
628 1-(2-Methoxyethyl)i-Pr 2,4-diF-Phenyl 94-97
629 1-(2,2-Diethoxyethyl)i-Pr 4-F-Phenyl oil*
630 1-(2,2-Diethoxyethyl)i-Pr 2,4-diF-Phenyl 84-88
631 1-(2-Methoxyethyl)i-Pr Phenyl oil*
632 1-(2,2-Diethoxyethyl)i-Pr Phenyl oil*
633 1-(2,2-Diethoxyethyl)i-Pr 4-CI-Phenyl 73-75
634 1-(2-Chloro-2-propenyl)i-Pr 2,4-diF-Phenyl oil*
635 n-Butyl i-Pr 2,4-diF-Phenyl oil*
636 n-Pentyl i-Pr 2,4-diF-Phenyl oil*
637 n-Hexyl i-Pr 2,4-diF-Phenyl oil*
638 MezNC(O)CHZCHZ i-Pr 4-F-Phenyl 100
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639 c-PrC(O)CHZ i-Pr 4-C1-Phenyl oil*
640 c-BuC(O)CHZ i-Pr 4-F-Phenyl oil*
641 c-BuC(O)CHZ i-Pr Phenyl 115-117
642 c-BuC(O)CHZ i-Pr 2,4-diF-Phenyl oil*
643 c-BuC(O)CH2 i-Pr 4-Cl-Phenyl oil*
644 (Et0)ZP(O)CH(CH3) i-Pr 4-Cl-Phenyl oil*
645 (2-Chloro-1,3,4-thiadiazol-5-i-Pr 2,4-diF-Phenyl 106-109
yl)methyl
646 (2-Chloro-1,3,4-thiadiazol-5-i-Pr 4-F-Phenyl I10-112
yl)methyl
647 1-(3-Cyanopropyl) i-Pr 4-F-Phenyl oil*
648 I-(2-t-Butyl-2-propenyl)i-Pr Phenyl oil*
649 1-(2-i-Propyl-2-propenyl)i-Pr Phenyl oil*
650 I-(2-Benzyl-2-propenyl)i-Pr Phenyl oil*
651 2-(3-Carbomethoxy-3-butenyl)i-Pr Phenyl oil*
652 1-(I-Ethynyl-3-methyl-2-i-Pr Phenyl oil*
butenyl)
653 (2-Chloro-1,3,4-thiadiazol-5-i-Pr 4-Cl-Phenyl oil*
yl)methyl
654 (2-Chloro-1,3,4-thiadiazol-5-i-Pr Phenyl oil*
yl)methyl
655 2-(4-Ethynyl-2-methyl-3-i-Pr Phenyl oil*
butenyl)
656 2-(5,6-Dihydro-1,2-Oxazin-3-i-Pr 4-F-Phenyl oil*
yl)ethyl
657 2-(3-Butynyl) i-Pr 2,4-diF-Phenyl oil*
658 2-(3-Butynyl) i-Pr 4-Cl-Phenyl oil*
659 (2-Tetrahydropyranyl)methyli-Pr Phenyl 97-100
660 (2-Tetrahydropyranyl)methyli-Pr 4-Cl-Phenyl 82-84
661 (3,4-Dihydroisoxazol-3-i-Pr 4-Cl-Phenyl 105-107
yl)methyl
662 (Me0)ZP(O)CHZCHZ i-Pr 4-F-Phenyl 79-85
663 i-Propyl i-Pr 4-Pyridyl 85-89
664 s-Butyl (S) i-Pr 4-Cl-Phenyl 53-56
665 s-Butyl (R) i-Pr 4-Cl-Phenyl 54-56
666 s-Butyl (S) i-Pr 2,4-diF-Phenyl 59-61
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667 s-Butyl(R) i-Pr 2,4-diF-Phenyl 58-60
668 1-(2-Fluoroethyl) i-Pr 4-CI-Phenyl 120-121
669 1-(2-Fluoroethyl) i-Pr Phenyl 88-89
670 1-(2-Fluoroethyl) i-Pr 2,4-diF-Phenyl 90-91
671 MeZNC(O)CHZCHZ i-Pr Phenyl 91
672 2-(1,3-Dichloropropyl)i-Pr 4-F-Phenyl oil*
673 1-(2,2-Dichloroethyl)i-Pr 2,4-diF-Phenyl 121-122
674 1-(3-Cyanopropyl) i-Pr Phenyl 89-92
675 1-(3-Cyanopropyl) i-Pr 2,4-diF-Phenyl oil*
676 (3,4-Dihydroisoxazol-3-i-Pr 2,4-diF-Phenyl 66-68
yl)methyl
677 PhCH(COZMe) i-Pr 4-F-Phenyl oil*
678 HOCHZCH2CH(COZMe) i-Pr Phenyl 120-123
679 HOCHzCHzCH(COzMe) i-Pr 4-Cl-Phenyl 107-110
680 HOCHzCH2CH(COZMe) i-Pr 4-F-Phenyl 102-106
681 EtO2CCHZCH(COZEt) i-Pr 4-Cl-Phenyl oil*
682 (1-Ethyl-5-Chloropyrazol-4-i-Pr 2,4-diF-Phenyl oil*
yl)methyl
683 (1-Ethyl-5-Chloropyrazol-4-i-Pr Phenyl oil*
yl)methyl
684 (1-Ethyl-5-Chloropyrazol-4-i-Pr 4-Cl-Phenyl oil*
yl)methyl
685 (I-Ethyl-5-Chloropyrazol-4-i-Pr 4-F-Phenyl oil*
yl)methyl
686 1-(1-Ethyl-5-Chloropyrazol-4-i-Pr 4-F-Phenyl oil*
yl)ethyl
687 Me2NC(O)CHZCHZ i-Pr 2,4-diF-Phenyl oil*
688 i-Propyl s-Butyl 4-F-Phenyl 59-61
(S)
689 i-Propyl s-Butyl 4-F-Phenyl 74-75
690 i-Propyl s-Butyl 4-F-Phenyl 64-65
(R)
691 i-Propyl i-Pr 4-Br-Phenyl 75-76
692 3-Cyclohexenyl i-Pr 4-F-Phenyl 80-82
693 HC(O)CH(CH3) i-Pr Phenyl oil*
694 3-Cyclohexenyl i-Pr 2,4-diF-Phenyl oil*
695 3-Cyclohexenyl i-Pr 4-CI-Phenyl 87-89
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696 3-Cyclohexenyl i-Pr ' Phenyl oil*
697 (Me0)zP(O)CHZCHz i-Pr Phenyl oil*
698 (Me0)zP(O)CHZCHz i-Pr 4-Cl-Phenyl oil*
699 1-(Cyclopropyl)ethyli-Pr Phenyl 65-67
700 1-(Cyclopropyl)ethyli-Pr 4-Cl-Phenyl 52-54
701 1-(Cyclobutyl)ethyli-Pr 4-CI-Phenyl oil*
702 1-(Cyclobutyl)ethyli-Pr 2,4-diF-Phenyl oil*
703 1-(Moipholinocarbonyl)ethyli-Pr 4-Cl-Phenyl 163
704 MezNC(S)CH(CH3) i-Pr Phenyl 141
705 1-(Morpholinocarbonyl)ethyli-Pr 4-F-Phenyl oil*
706 (3,4-Dihydroisoxazol-3-i-Pr Phenyl oil*
yl)methyl
707 2-(1-Chloro-3-fluoropropyl)i-Pr 4-F-Phenyl 85-86
708 2-(1-Acetoxy-3-chloropropyl)i-Pr 2,4-diF-Phenyl oil*
709 Fluoromethyl i-Pr 4-F-Phenyl 126-127
710 2,2-Difluoroethyl i-Pr 4-F-Phenyl 94-96
711 2,2-Difluoroethyl i-Pr 2,4-diF-Phenyl 105-108
712 1-(4-Chlorobutyl) i-Pr 4-F-Phenyl oil*
713 1-(3-Chloropropyl)i-Pr 4-F-Phenyl oil*
714 1-(2-Chloropropyl)i-Pr 2,4-diF-Phenyl oil*
(S)
715 (2-Tetrahydropyranyl)methyli-Pr 2,4-diF-Phenyl oil*
716 (2-Phenyl-1,3,4-oxadiazol-S-i-Pr Phenyl 130-132
yl)methyl
717 1-(Cyclobutyl)ethyli-Pr Phenyl oil*
718 1-(Cyclobutyl)ethyli-Pr 4-F-Phenyl oil*
719 MezNC(O)CHzCHz i-Pr 4-Cl-Phenyl 82-83
720 1-(Cyclopropyl)ethyli-Pr 2,4-diF-Phenyl oil*
721 1-(3,4-Dihydroisoxazol-3-i-Pr 4-F-Phenyl oil*
yl)ethyl
722 (5-Phenyl-1, 2, i-Pr Phenyl 120-121
5-oxadiazol-2-
yl)methyl
723 PhCH(COZMe) i-Pr Phenyl oil*
724 PhCH(COZMe) i-Pr 4-Cl-Phenyl oil*
725 1-(2-Chloro-1-methoxyethyl)i-Pr 4-Cl-Phenyl oil*
726 1-(1,2-Dimethoxyethyl)i-Pr 4-Cl-Phenyl oil*
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727 CH3C(O)NHCHZCHZ i-Pr 4-F-Phenyl oil*
728 MeZNC(S)CH(CH3) i-Pr 4-F-Phenyl 130
729 1-(3,4-Dihydroisoxazol-3-i-Pr Phenyl oil*
yl)ethyl
730 1-(3,4-Dihydroisoxazol-3-i-Pr 2,4-diF-Phenyl oil*
yl)ethyl
731 1-(2-(6-Chloro-2-pyridyl)-2-i-Pr Phenyl oil*
propenyl)
732 1-(2-Carbomethoxy-2-propenyl)i-Pr 4-F-Phenyl oil*
733 Me2NC(S)CH(CH3) i-Pr 4-Cl-Phenyl 136
734 1-(1,2-Dimethoxyethyl)i-Pr Phenyl oil*
735 1-(2-Chloro-1-methoxyethyl)i-Pr Phenyl oil*
736 (Et0)ZP(O)CHZ i-Pr 2,4-diF-Phenyl 113-115
737 1-(2-Chloro-1-methoxyethyl)i-Pr 2,4-diF-Phenyl oil*
738 1-(1,2-Dimethoxyethyl)i-Pr 2,4-diF-Phenyl oil*
739 MeZNC(S)CH(CH3) i-Pr 2,4-diF-Phenyl 107
740 (5,6-Dihydro-1,2,4-Dioxazin-3-i-Pr 4-CI-Phenyl 107
yl)methyl
741 PhCON(CH3)CHzCH2 i-Pr 4-F-Phenyl 141-146
742 1-(1-Ethoxypropyl)i-Pr 4-F-Phenyl oil*
743 Propargyl i-Pr 4-F-Phenyl oil*
744 1-(3-Butynyl) i-Pr 2,4-diF-Phenyl oil*
745 2,2-Difluoroethyl i-Pr 4-Cl-Phenyl 104-107
746 2,2-Difluoroethyl i-Pr Phenyl oil*
747 1-(2-Chloropropyl)i-Pr Phenyl oil*
(S)
748 1-(2-Chloropropyl)i-Pr 4-Cl-Phenyl oil*
(S)
749 1-(3-Chloropropyl)i-Pr 4-Cl-Phenyl 68-72
750 1-(3-Chloropropyl)i-Pr Phenyl oil*
751 s-Hutyl i-Pr 4-F-Phenyl 42-44
752 1-(3-Bromo-2-methylpropyl)i-Pr 4-F-Phenyl 96-100
753 3-(4-Pentynyl) i-Pr 4-F-Phenyl oil*
754 Propargyl i-Pr Phenyl 75-76
755 Bromomethyl i-Pr Phenyl 82-84
756 1-(4,5-Dimethylthiazol-2-i-Pr Phenyl 101-104
yl)ethyl
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757 1-(4,5-Dimethylthiazol-2-i-Pr 4-F-Phenyl 103-105
yl)ethyl
758 (5,6-Dihydro-1,2,4-Dioxazin-3-i-Pr 2,4-diF-Phenyl oil*
yl)methyl
759 I-(3,4-Dihydroisoxazol-3-i-Pr 4-CI-Phenyl oil*
yl)ethyl
760 (5,6-Dihydro-6-OMe-1,2-i-Pr 4-CI-Phenyl 107-109
oxazin-3-yl)methyl
761 PhCON(CH3)CHZCHZ i-Pr Phenyl 124-127
762 PhCON(CH3)CHZCHZ i-Pr 2,4-diF-Phenyl 106-108
763 2-(3-Butynyl) i-Pr 4-F-Phenyl oil*
764 Propargyl i-Pr 2,4-diF-Phenyl oil*
765 (5,6-Dihydro-1,2,4-Dioxazin-3-i-Pr 4-F-Phenyl oil*
yl)methyl
766 (Dihydro-6-OMe-1,2-oxazin-3-i-Pr 4-F-Phenyl oil*
yl)methyl
767 1-(3-Butynyl) i-Pr 4-F-Phenyl oil*
768 1-(3-Butynyl) i-Pr Phenyl oil*
769 (5-i-Propyl-1, 2, i-Pr Phenyl oil*
5-oxadiazol-2-
yl)methyl
770 (5-c-Hexyl-1, 2, i-Pr Phenyl 106-108
5-oxadiazol-2-
yl)methyl
771 i-Propyl i-Pr 2-Cl-5-Pyridiyl oil*
772 1-(1-Ethoxypropyl) i-Pr 4-CI-Phenyl oil*
773 1-( 1-Ethoxypropyl)i-Pr Phenyl oil*
774 1-(1-Ethoxypropyl) i-Pr 2,4-diF-Phenyl oil*
775 CH302CN(CH3)CHZCHZ i-Pr Phenyl oil*
776 (Et0)ZP(O)CH(CH3) i-Pr 2,4-diF-Phenyl oil*
777 (CH30)ZP(O)CHZCHZ i-Pr 2,4-diF-Phenyl oil*
778 CH302CN(CH3)CHZCHZ i-Pr 2,4-diF-Phenyl oil*
779 CH30zCN(CH3)CHZCHz i-Pr 4-CI-Phenyl oil*
780 i-Propyl i-Pr 4-OMe-Phenyl 93-94
781 1-(3-Methyl-3-nitropropyl)i-Pr 2,4-diF-Phenyl 118-120
782 1-(3, 3-Dichloro-2-propenyl)i-Pr 4-F-Phenyl oil*
783 3-(4-Pentynyl) i-Pr 2,4-diF-Phenyl oil*
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784 Propargyl i-Pr 4-CI-Phenyl oil*
785 1-(4,5-Dimethylthiazol-2-i-Pr 2,4-diF-Phenyl oil*
yl)ethyl
786 Pyrrolidinothiocarbonylmethyli-Pr 2,4-diF-Phenyl 68
787 Pyn olidinothiocarbonylmethyli-Pr 4-Cl-Phenyl 144
788 Pyrrolidinothiocarbonylmethyli-Pr Phenyl 117
789 Pyrrolidinothiocarbonylmethyli-Pr 4-F-Phenyl 142
790 2-(3-Methoximinopropyl)i-Pr Phenyl 82-87
791 1-(4-Chlorobutyl) i-Pr 4-Cl-Phenyl 103-109
792 1-(4-Chlorobutyl) i-Pr Phenyl oil*
793 4-Cyclohexenyl i-Pr 4-F-Phenyl 107-108
794 1-(2-Bromoethyl) i-Pr 4-F-Phenyl 105-106
795 1-(2-Bromoethyl) i-Pr 2,4-diF-Phenyl 77-80
796 1-(2-Bromoethyl) i-Pr 4-CI-Phenyl 85-87
797 (Pinenyl)methyl i-Pr Phenyl oil*
798 i-Propyl i-Pr (3,5-Dimethylisoxazol-4-oil*
yl)methyl
799 1-(2,2-Dimethylcyclopropyl)i-Pr 4-F-Phenyl 69-72
800 1-(2,2-Dimethylcyclopropyl)i-Pr Phenyl oil*
801 1-(2,2-Dimethylcyclopropyl)i-Pr 4-CI-Phenyl oil*
802 1-(2,2-Dimethylcyclopropyl)i-Pr 2,4-diF-Phenyl oil*
803 3-(4-Pentynyl) i-Pr Phenyl oil*
804 1-(3-Butynyl) i-Pr 4-Cl-Phenyl oil*
805 2-(1,3-Dibromopropyl)i-Pr 4-F-Phenyl oil*
806 1-(3-Bromo-2,2- i-Pr 4-F-Phenyl 122-126
dimethylpropyl)
807 (5,6-Dihydro-6-methoxy-1,2-i-Pr 2,4-diF-Phenyl 110-115
oxazin-3-yl)methyl
808 3-(4-Pentynyl) i-Pr 4-Cl-Phenyl oil*
809 (5,6-Dihydro-6-methoxy-1,2-i-Pr Phenyl 96-98
oxazin-3-yl)methyl
810 1-(4,5-Dihydro-5- i-Pr 4-F-Phenyl oil*
methoxyisoxazol-3-yl)ethyl
811 1-(4,5-Dihydroisoxazol-S-i-Pr 4-F-Phenyl oil*
yl)ethyl
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812 1-(4,5-Dihydro-5- i-Pr Phenyl oil*
methoxyisoxazol-3-yl)ethyl
813 i-Pr c-PrCH2 4-F-Phenyl 76 -77
814 1-(4,5-Dihydroisoxazol-5-i-Pr 4-Cl-Phenyl oil*
yl)ethyl
815 1-(4,5-Dihydroisoxazol-5-i-Pr 2,4-diF-Phenyl oil*
yl)ethyl
816 1-(4,5-Dihydroisoxazol-5-i-Pr Phenyl oil*
yl)ethyl
817 2-(1,1,1-Trifluoropropyl)i-Pr 2,4-diF-Phenyl oil*
818 3-( 1-Trimethylsilylpropyl)i-Pr 4-F-Phenyl oil
819 1-(2,3-Epoxy-2-methylpropyl)i-Pr 4-F-Phenyl oil*
820 1-(2,3-Epoxy-2-methylpropyl)i-Pr 4-F-Phenyl 78 -
(S) 80
821 (MeOzC)ZCH i-Pr Phenyl oil
822 1-(3-Chloropropyl)i-Fr 2,4-diF-Phenyl oil*
823 1-(4-Chlorobutyl) i-Pr 2,4-diF-Phenyl oil*
824 2-(3-Chloro-3-methoxypropyl)i-Pr Phenyl oil*
825 2-(3-Chloro-3-methoxypropyl)i-Pr 4-F-Phenyl oil*
826 1-(2,2-Dichloroethyl)i-Pr 4-F-Phenyl 95 -
98
827 1-(2-Butynyl) i-Pr 2,4-diF-Phenyl 131 -
132
828 1-(2-Butynyl) i-Pr 4-F-Phenyl 115 -
116.5
829 i-Pr i-Pr (5-t-Butyl-1,2,4-oxadiazol-oil*
3-yl)methyl
830 1-(2-Butynyl) i-Pr 4-Cl-Phenyl 24 -
25
831 1-(2-Cyclopropylethyl)i-Pr 4-F-Phenyl 70 -
72
832 1-(2-Cyclopropylethyl)i-Pr Phenyl 70 -
72
833 1-(2-Butynyl) i-Pr Phenyl 90.5
- 92
834 1-(1,3-Dioxolan-2-yl)ethyli-Pr 4-F-Phenyl 104 -
107
835 1-(1,3-Dioxan-2-yl)ethyli-Pr 4-F-Phenyl 94 -
96
836 1-(5,5-Dimethyl-1,3-dioxan-2-i-Pr 4-F-Phenyl 90 -
yl)ethyl 93
837 1 -(1,3-Dioxepin-5-en-2-yl)ethyli-Pr 4-F-Phenyl oil*
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838 i-Pr i-Pr 2,6-DiF-Phenyl 80 -
83
839 i-Pr i-Pr 2,3-DiF-Phenyl oil*
840 i-Pr Et 4-F-Phenyl oil*
841 2-(3-Butenyl) i-Pr 4-C1-Phenyl oil*
842 2-(3-Butenyl) i-Pr 2,4-diF-Phenyl oil*
843 2-(3-Butenyl) i-Pr Phenyl oil*
844 1-(3-Methylenecyclobutane)i-Pr 4-F-Phenyl 60 -
61
845 1-(3-Methylenecyclobutane)i-Pr 2,4-diF-Phenyl oil*
846 1-(3-Methylenecyclobutane)i-Pr Phenyl oil*
847 1-(3-Methylenecyclobutane)i-Pr 4-CI-Phenyl 81- 84
848 3-Cyclopentene i-Pr 4-F-Phenyl 71 -
74
849 HC(O)CH(CH3) i-Pr 4-CI-Phenyl oil*
850 HC(O)CH(CH3) i-Pr Phenyl oil*
851 (3-Chloro-1-methylpyrazol-4-i-Pr 4-F-Phenyl 105 -
yl)methyl 107
852 (3-Chloro-1-methylpyrazol-4-i-Pr 4-Cl-Phenyl oil*
yl)methyl
853 (3-Chloro-1-methylpyrazol-4-i-Pr Phenyl oil*
yl)methyl
854 (3-Chloro-1-methylpyrazol-4-i-Pr 2,4-diF-Phenyl oil*
yl)methyl
855 (1-Methyl-5-chloro-3-i-Pr Phenyl 152 -
trifluoromethylpyrazol-4- 154
yl)methyl
856 (1-Methyl-S-chloro-3-i-Pr 4-F-Phenyl 148 -
trifluoromethylpyrazol-4- 149
yl)methyl
857 (1-Methyl-5-chloro-3-i-Pr 2,4-diF-Phenyl 112 -
tiifluoromethylpyrazol-4- 114
yl)methyl
858 (1-Methyl-5-chloro-3-i-Pr 4-CI-Phenyl 132 -
trifluoromethylpyrazol-4- 136
yl)methyl
859 (1-Methyl-4-bromopyrazol-3-i-Pr Phenyl 161 -
yl)methyl 165
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860 (1-Methyl-4-bromopyrazol-3-i-Pr 4-F-Phenyl 124
yl)methyl - 132
861 1-(1-Methyl-4-bromopyrazol-3-i-Pr Phenyl 123
yl)ethyl - 124
862 1-(1-Methyl-4-bromopyrazol-3-i-Pr 4-F-Phenyl 122
yl)ethyl - 124
863 (1-Methyl-4-bromopyrazol-3-i-Pr 4-Cl-Phenyl 147
yl)methyl - 150
864 1-(1-Methyl-4-bromopyrazol-3-i-Pr 4-Cl-Phenyl 119
yl)ethyl - 121
865 (1-Methyl-4-bromopyrazol-3-i-Pr 2,4-diF-Phenyl 116
yl)methyl - 117
866 1-(1-Methyl-4-bromopyrazol-3-i-Pr 2,4-diF-Phenyl oil*
yl)ethyl
867 Cyclooctyl i-Pr 4-F-Phenyl 81 -
84
868 i-Pr 2-(3-Me0-propyl)Phenyl 73 -
77
869 i-Pr 2-(3-Me0-propyl)4-F-Phenyl 119
- 125
870 i-Pr 2-(3-Me0-propyl)4-Cl-Phenyl 76 -
81
871 2-(3-Chloro-3-methoxypropyl)i-Pr 4-Cl-Phenyl oil*
872 2-(3-Chloro-3-methoxypropyl)i-Pr 2,4-diF-Phenyl oil*
873 1-(2,2-Dichloroethyl)i-Pr 4-Cl-Phenyl 80 -
88
874 1-(2,2-Dichloroethyl)i-Pr Phenyl 95 -
96
875 1-(2-Chloropropyl)i-Pr 4-F-Phenyl 55 -
(S) 60
876 2-(1,1,1-Trifluoropropyl)i-Pr 4-Cl-Phenyl -
877 Cyclooctyl i-Pr Phenyl 50 -
58
878 i-Pr Allyl Phenyl 58 -
60
879 Cyclooctyl i-Pr 4-Cl-Phenyl 99 -
103
880 Cyclooctyl i-Pr 2,4-diF-Phenyl 89 -
93
881 MezNC(O)OCHZCHZ i-Pr 4-F-Phenyl 94 -
96
882 3-(1-Hexynyl) i-Pr Phenyl oil*
883 i-Pr (CD3)ZCH 4-F-Phenyl 66 -
68
884 1-(3-Allyloxy-2- i-Pr 4-F-Phenyl oil*
methoximinopropyl)
885 1-(3-Allyloxy-2- i-Pr Phenyl oil*
methoximinopropyl)
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886 1-(3-Allyloxy-2- i-Pr 2,4-diF-Phenyl oil*
methoximinopropyl)
887 1-(3-Allyloxy-2- i-Pr 4-CI-Phenyl oil*
methoximinopropyl)
888 i-Pr 2-(1-Chloropropyl)4-Cl-Phenyl oil*
889 (1,3-Dioxolan-4-yl)methyli-Pr 4-F-Phenyl 75 -
78
890 (2,2-Dimethyl-1,3-dioxolan-4-i-Pr 4-F-Phenyl 110
yl)methyl - 113
891 (1,3-Dioxolan-4-yl)methyli-Pr Phenyl 91 -
96
892 2-Methoxymethylpyrrolidin-1-i-Pr 4-F-Phenyl oil*
yl
893 1-(3-Methylbutyl) i-Pr Phenyl 63 -
65
894 1-(3-Methylbutyl) i-Pr 4-Cl-Phenyl 64 -
66
895 1-(3-Methylbutyl) i-Pr 4-F-Phenyl 88 -
91
896 1-(3-Methylbutyl) i-Pr 2,4-diF-Phenyl 54 -
56
897 3-(1-Hexynyl) i-Pr 2,4-diF-Phenyl 63 -
64
898 1-(1,3-Dioxepin-2-yl)ethyli-Pr 4-F-Phenyl oil*
899 (1,3-Dioxolan-2-yl)methyli-Pr 4-F-Phenyl 84 -
87
900 1-(3-Henzyloxy-2- i-Pr 4-F-Phenyl oil*
methoximinopropyl)
901 1-(3-Benzyloxy-2- i-Pr Phenyl oil*
methoximinopropyl)
902 1-(3-Methoxy-2- i-Pr 4-F-Phenyl oil*
methoximinopropyl)
903 1-(3-Methoxy-2- i-Pr Phenyl oil*
methoximinopropyl)
904 1-(3-Methoxy-2- i-Pr Phenyl. oil*
methoximinopropyl)
905 i-Pr 2-(1,1- 4-CI-Phenyl oil*
Dimethoxypropyl)
906 i-Pr 2-(1-Chloropropyl)Phenyl 92 -
94
907 i-Pr 2-(1-Chloropropyl)4-F-Phenyl 95 -
97
908 i-Pr 2-(3-Chlorobutyl)Phenyl oil*
909 i-Pr 2-(3-Chlorobutyl)4-F-Phenyl oil*
910 i-Pr n-Bu 4-F-Phenyl 72 -
73
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911 i-Pr n-Pr 4-F-Phenyl 63 -
64
912 i-Pr i-Bu 4-F-Phenyl 66 -
67
913 CH3C(O)CHZCHZ i-Pr Phenyl oil*
914 HC(O)CHZCHZ i-Pr 4-F-Phenyl oil*
915 CH3C(O)CHZCHZCHZ i-Pr 2,4-diF-Phenyl oil*
916 CH3C(O)CHZCH2CH2 i-Pr 4-Cl-Phenyl oil*
917 3-(1-Hexynyl) i-Pr 4-Cl-Phenyl oil*
918 i-Pr 2-(1,1,1- Phenyl 92 -
Trifluoropropyl) 94
919 i-Pr 2-(1,1- Phenyl oil*
Dimethoxypropyl)
920 i-Pr 2-(1,1- 4-F-Phenyl oil*
Dimethoxypropyl)
921 i-Pr 1-(1-Cyanoethyl)4-F-Phenyl 80 -
82
922 1-(3-Methoxy-2- i-Pr 4-Cl-Phenyl oil*
methoximinopropyl)
923 1-(3-Methoxy-2- i-Pr 2,4-diF-Phenyl oil*
methoximinopropyl)
924 i-Pr Allyl 4-F-Phenyl 57 -
59
925 i-Pr c-Hexyl 4-F-Phenyl 126 -
131
926 i-Pr c-Pentyl 4-F-Phenyl 93 -
95
927 3-(Cyclopentene) i-Pr 2,4-diF-Phenyl oil*
928 3-(Cyclopentene) i-Pr 4-Cl-Phenyl 100 -
103
929 3-(Cyclopentene) i-Pr Phenyl oil*
930 1-(3-Oxocyclobutyl)i-Pr 4-F-Phenyl oil*
931 1-(3-Oxocyclobutyl)i-Pr 2,4-diF-Phenyl 95 -
97
932 1-(3-Oxocyclobutyl)i-Pr Phenyl 148 -
150
933 1-(3-Oxocyclobutyl)i-Pr 4-Cl-Phenyl 120 -
122
934 CH3C(O)CHZCHZ i-Pr 4-F-Phenyl 94 -
95
935 CH3C(O)CHZCHZ i-Pr 2,4-diF-Phenyl oil*
936 CH3C(O)CHzCH2 i-Pr 4-Cl-Phenyl 111 -
113
937 1-(3-Butenyl) i-Pr 4-F-Phenyl 40 -
42
938 1-(3-Butenyl) i-Pr 2,4-diF-Phenyl 58 -
60
939 1-(3-Butenyl) i-Pr Phenyl 43 -
45
940 1-(3-Butenyl) i-Pr 4-Cl-Phenyl 50 -
51
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941 i-Pr Neopentyl 4-F-Phenyl 88 -
89
942 i-Pr (CH3)3CCH2 4-F-Phenyl 79 -
CHZ 80
943 2-(1-Chloro-3-Fluoropropyl)i-Pr 4-CI-Phenyl 87 -
90
944 2-(1,3-Dichloropropyl)i-Pr 4-Cl-Phenyl 79 -
82
945 4-(2,3,5,6- i-Pr 4-F-Phenyl 163 -165
Tetrahydrothiopyranyl)
946 4-(2,3,5,6- i-Pr Phenyl 145 -148
Tetrahydrothiopyranyl)
947 4-(2,3,5,6- i-Pr 2,4-diF-Phenyl oil*
Tetrahydrothiopyranyl)
948 4-(2,3,5,6- i-Pr 4-CI-Phenyl 153 -
Tetrahydrothiopyranyl) 157
949 3-(2,3,4,5-Tetrahydrothienyl)i-Pr 4-F-Phenyl 67 -70
950 2-(1-Chloro-3-Fluoropropyl)i-Pr Phenyl 100-
103
951 i-Pr 3-(2,3,4,5- 4-F-Phenyl 114 -117
Tetrahydrothienyl)
952 i-Pr N=CHMe Phenyl oil*
953 i-Pr N~Me2 Phenyl oil*
954 PyrrolidinoC(O)OCHZCHZi-Pr Phenyl 100 -
104
955 i-Pr 2-(1,3-DiCI-propyl)Phenyl oil*
956 i-Pr 2-(1,3-DiCI-propyl)4-F-Phenyl oil*
957 i-Pr 3-(2-Me-butyl)4-F-Phenyl 109 -
110
958 c-Pr (CD3)ZCH 4-F-Phenyl 69 -
70
959 3-(2-Methyl-4-pentynyl)i-Pr Phenyl oil*
960 EtOC(O)OCHZCHz i-Pr 4-F-Phenyl 105-108
961 i-Pr 3-Pentyl 4-F-Phenyl 55 -
57
962 CH3C(O)CHZCHZCHZ i-Pr 4-F-Phenyl oil*
963 CH3C(O)CHZCHZCHz i-Pr Phenyl oil*
964 HC(O)CHZCHZ i-Pr 2,4-diF-Phenyl oil*
965 HC(O)CHZCHZ i-Pr Phenyl oil*
966 HC(O)CHzCHz i-Pr 4-Cl-Phenyl 98 -
100
967 4-(1-Hexynyl) i-Pr 4-F-Phenyl oil*
*see Index Table D for 1H NMR data.
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INDEX TABLE D
Cmpd . 1 H NMR Data (CDCl3 solution unless indicated otherwise)a
No
77 S 7.30 (d, 1H), 7.20 (d, 1H), 6.99 (m, 1H), 4.89 (s, 2H),
3.50 (q, 4H), 1.24 (t, 6H).
80 8 7.22 (m, 4H), 7.09 (m, 2H), 6.96 (m, 1H), 4.78 (s, 2H),
4.42 (m, 1H), 1.20 (d, 6H).
82 8 7.32 (d, 1H), 7.20 (d, 1H), 7.00 (m, 1H), 4.90 (s, 2H),
3.95 (m, 1H), 3.40 (m, 2H), 1.82 (m, 4H),
1.70-1.50 (m, 2H), 1.40-1.20 (m, 7H).
83 S 7.3 (d, 1H), 7.19 (d, 1H), 6.96 (m, 1H), 4.88 (s, 2H),
4.38 (m, 1H), 4.20 (s, 2H), 3.80 (t, 2H) 2.30
(br.s, 2H), 1.28 (d, 6H).
84 8 7.41 (d, 1H), 7.10 (m, 4H), 4.75 (s, 2H), 3.50 (q, 4H),
3.45 (s, 3H), 1.24 (t, 6H).
85 b 7.41-7.14 (m, 9H), 4.66 (s, 2H), 3.44 (s, 3H), 2.37
(s, 3H).
87 8 7.38 (m, 1H), 7.10 (m, 4H), 6.92 (m, 2H), 4.64 (m, 3H),
2.36 (s, 3H), 1.10 (m, 6H).
90 S 7.10 (m, 8H), 5.20 (m, 1H), 4.60 (m, 1H), 2.80 (m, 3H),
2.20 (m, 2H) 1.20 (d, 6H).
91 8 7.22 (m, 2H), 7.08 (m, 2H), 4.62 (m, 1H), 3.42 (t, 2H),
1.62 (m, 2H), 1.20 (d, 6H), 0.90 (t, 3H).
92 8 7.40 (m, 2H), 7.12 (m, 2H), 4.64 (m, 1H), 3.42 (t, 2H),
1.62 (m, 2H), 1.20 (d, 6H), 0.90 (t, 3H).
99 b 7.3 (m, 2H), 7.1 (m, 2H), 4.7 (m, 1H), 4, 1 (m, 1H),
2.4-2.7 (m, 2H), 2.2 (m, 1H), 2.0 (m, 1H),
1.3-1.8 (m SH), 1.2 (d, 6H).
101 b 6.87 (t, 2H), 6.52 (dd, 2H), 3.57 (m, 1H), 2.91 (q,
2H), 2.70 (s, 3H), 1.32 (t, 3H), 1.19 (d, 6H).
105 8 7.40 (d, 2H), 7.20 (d, 2H), 5.80 (m, 1H), 5.30 (m, 2H),
4.04 (d, 2H), 1.20 (d, 6H).
106 S 7.40-7.08 (m, 9H), 4.40 (m, 3H), 1.20 (d, 6H).
115 8 7.40 (d, 2H), 7.10 (d, 2H), 4.62 (m, 1H), 3.42 (t, 2H),
1.64 (q, 2H), 1.20 (d, 6H), 0.92 (t, 3H).
126 b 5.87 (br m, 1H), 4.41 (m, 1H), 4.27 (m, 2H), 3.86 (t,
2H), 2.41 (s, 3H), 2.35 (br m, 2H), 2.25 (s,
3H), 1.32 (d, 6H).
127 8 7.3 (m, 1H), 6.8-7.0 (m, 2H), 5.7-5.9 (m, 1H), 5.2-5.4
(t, 2H), 4.1 (d, 2H), 3.3 (m, 1H), 1.3 (m,
2H), 0.7 (d, 2H).
128 8 7.2-7.4 (m, 4H), 7.1 (t, ZH), 4.8 (m, 1H), 4.2 (g, 4H),
4.0 (s, 2H), 1.3 (t, 6H), 1.1 (d, 6H).
129 8 7.40-7.20 (m, SH), 4.62 (m, 1H), 3.42 (t, 2H), 1.58
(s, 9H), 1.20 (d, 6H).
130 8 7.38 (m, 1H), 6.94 (m, 2H), 4.64 (m, 1H), 3.43 (t, 2H),
1.62 (m, 2H), 1.20 (m, 6H), 0.90 (t, 3H).
133 b 7.40-7.18 (m, 9H), 5.18 (q, 1H), 4.40 (m, 1H), 1.80
(d, 3H), 1.18 (d, 6H).
134 8 7.40-7.10 (m, 9H), 5.18 (q, 1H), 4.42 (m, 1H), 1.80
(d, 3H), 1.18 (d, 6H).
135 8 7.27 (m, 2H ), 7.11 (t, 2H), 4.69 (m, 1H), 2.92 (m,
1H), 2.76 (m, 1H), 1.32-1.14 (m, 18H).
144 b 7.40-7.27 (m, 8H), 5.80 (s, 1H), 4.86 (s, 2H), 4.40
(m, 1H), 4.22 (s, 2H), 3.80 (t, 2H), 2.30 (s, 2H),
1.28 (d, 6H).
145 8 7.40-7.27 (m, 4H), 5.80 (br.s, 1H), 4.86 (s, 2H), 4.30
(m, 1H), 2.38 (m, 1H), 2.16 (m, 4H), 1.90
(m, 1H), 1.70 (m, 2H), 1.26 (d, 6H).
147 8 5.8 (m, 2H), 5.38 (m, 2H), 4.4 (m, 1H), 4.22 (s, 2H),
4.08 (m, 2H), 3.83 (t, 2H), 2.30 (br.s, 2H),
1.26 (d, 6H).
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148 b 7.22 (m, 2H), 7.10 (m, 2H), 4.40 (m, 1H), 3.80-3.50 (m,
4H), 1.21 (d, 6H).
149 b 5.72 (s, 1H), 4.40 (m, 1H), 4.28 (s, 2H), 4.16 (m, 2H),
7.10 (m, 2H), 4.40 (m, 1H), 3.80-3.50 (m,
4H), 1.21 (d, 6H).
150 8 5.82 (s, 1H), 5.38 (m, 2H), 4.18 (d, 2H), 3.72 (br.s,
2H), 3.54 (br.s, 2H), 1.96 (br.s, 4H).
151 8 7.30 (m, 1H), 6.92 (m, 2H), 5.80 (m, 1H), 5.26 (m, 2H),
4.42 (m, 1H), 4.06 (d, 2H), 1.2 (m, 6H).
152 b 7.40 (m, SH), 4.71 (s, 2H), 3.50 (q, 4H), 1.24 (t, 6H).
153 8 7.31 (m, lOH), 4.61 (s, 2H), 3.43 (s, 3H).
172 8 7.40 (m, 1H), 6.94 (m, 2H), 4.62 (m, 1H), 4.02 (m, 1H),
3.40 (m, 1H), 1.20 (m, 6H), 0.78 (d, 3H).
174 8 7.20-7.40 (m, 4H), 5.02 (m, 1H), 4.62 (m, 1H), 1.80 (d,
3H), 1.18 (d, 6H).
178 8 7.40-7.20 (m, 4H), 4.62 (m, 1H), 3.40 (m, 1H), 1.20 (d,
6H), 0.78 (d, 3H).
180 b 7.3 (m, 1H), 7.2-7.1 (d, 2H), 5.1-5.0 (m, 1H), 3.99 (s,
6H), 2.22 (s, 6H), 1.46 (d, 6H).
181 8 7.5-7.1 (m, 4H), 5.1-5.0 (m, 1H), 4.00 (s, 6H), 2.26
(s, 3H), 1.5 (d, 6H).
182 8 5.0 (m, 1H), 4.3 (m, 1H), 3.97 (s, 6H), 1.5-1.4 (m, 12H).
183 8 7.3 (m, 2H), 7.0 (m, 1H), 6.8 (m, 2H), 3.9 (m, 1H), 3.4
(m, SH), 1.9-1.1 (m, 13H).
184 8 7.2 (m, 2H), 7.1 (m, 2H), 4.6 (m, 1H), 4.1-3.8 (m, 1H),
2.2-1.7 (m, 9H), 1.2 (d, 6H).
188 8 7.25 (m, 2H), 7.10 (m, 2H), 4.65 (m, 1H), 3.65 (m, 2H),
3.20 (m, 1H), 2.80 (t, 1H), 2.62 (m, 1H),
1.21 (d, 6H).
189 8 8.6 (m, 2H), 7.2 (m, 2H), 4.69 (s, 2H), 4.3 (m, 1H),
3.5 (bm, 2H), 1.50 (d, 6H), 1.22 (t, 3H).
190 8 8.97 (s, 1H), 4.6 (q, 2H), 4.4 (m, 1H), 1.5 (m, 9H).
191 b 7.37 (d, 2H), 7.19 (d, 2H), 4.70 (s, 2H), 4.55-4.67 (m,
1H), 2.61 (s, 3H), 2.42 (s, 3H), 1.20 (d, 6H).
192 8 7.20-7.25 (m, 2H), 7.04-7.10 (m, 2H), 4.70 (s, 2H), 4.58-4.67
(m, 1H), 2.61 (s, 3H), 2.42 (s, 3H),
1.19 (d, 6H).
196 8 7.38-7.41 (m, 2H), 7.20-7.23 (m, 2H), 4.62-4.71 (m, 1H),
2.66 (s, 3H), 2.21 (s, 3H), 1.23 (d, 6H).
197 8 7.41-7.43 (m, 3H), 7.25-7.28 (m, 2H), 4.61-4.74 (m, 1H),
2.65 (s, 3H), 2.19 (s, 3H), 1.24 (d, 6H).
198 8 7.24-7.28 (m, 2H), 7.11 (t, 2H), 4.61-4.74 (m, 1H), 2.66
(s, 3H), 2.21 (s, 3H), 1.23 (d, 6H).
201 8 7.4 (m, 3H), 7.2-7.25 (m, 3H), 7.1-7.2 (t, 2H), 4.6-4.8
(m, 1H), 2.3-2.4 (q, 2H), 2.07 (s, 3H), 1.2
(d, 6H), 1.0 (t, 3H).
206 b 7.40-7.20 (m, SH), 6.40 (m, 1H), 6.36 (m, 1H), 4.60 (m,
3H), 1.20 (d, 6H).
207 8 7.40 (s, 1H) 7.20 (m, 2H), 7.18 (m, 2H), 4.60 (m, 3H),
1.20 (d, 6H).
208 8 7.40 (m, 2H), 6.94 (t, 2H), 6.38 (m, 1H), 6.36 (m, 1H),
4.62 (m, 3H), 1.20 (d, 6H).
210 8 7.29 (m, 7H), 7.17 (m, 2H), 6.65 (d, 1H), 6.1 (m, 1H),
4.65 (m, 1H), 4.22 (d, 2H), 1.2 (d, 6H).
213 8 7.23 (m, 2H), 7.09 (m, 2H), 4.65 (m, 1H), 4.24 (s, 2H),
1.2 (d, 6H), 0.14 (s, 9H).
214 8 7.24 (m, 2H), 7.1 (m, 2H), 6.75 (m, 1H), 5.92 (m, 1H),
4.65 (m, 1H), 4.2 (m, 4H), 1.28 (t, 3H), 1.2
(d, 6H).
215 8 7.23 (m, 2H), 7.09 (m, 2H), 4.65 (m, 1H), 4.21 (s, 2H),
3.77 (s, 3H), 1.2 (d, 6H).
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216 8 7.27 (m, 2H), 7.08 (m, 2H), 4.65 (m, 1H), 4.38 (s, 2H),
1.21 (m, 15H).
217 8 7.2 (m, 2H), 7.1 (m, 2H), 4.65 (m, 1H), 4.25 (s, 2H),
2.22 (s, 3H), 1.2 (d, 6H).
218 8 7.23 (m, 2H), 7.11 (m, 2H), 4.65 (m, 1H), 3.7 (t, 2H),
2.65 (m, 2H), 1.2 (d, 6H).
220 b 7.23 (m, 2H), 7.09 (m, 2H), 4.65 (m, 1H), 3.68 (m, 4H),
3.55 (m, 2H), 3.44 (m, 2H), 3.31 (s, 3H),
1.2 (d, 6H).
221 8 7.22 (m, 2H), 7.09 (m, 2H), 4.65 (m, 1H), 3.47 (t, 2H),
1.6 (m, 2H), 1.3 (m, 2H), 1.2 (d, 6H), 0.9
(t, 3H).
222 b 7.40 (m, 1H), 6.90 (m, 2H), 4.70 (m, 1H), 3.71 (s, 3H),
2.31 (s, 3H), 2.10 (s, 3H), 1.20 (m, 6H).
223 S 7.26 (m, 2H), 7.15 (m, 4H), 6.70 (m, 1H), 2.33 (s, 3H),
2.15 (s, 3H), 1.20 (m, 6H).
225 8 7.40 (m, 3H), 7.30 (m, 2H), 4.65 (m, 1H), 2.80 (s, 6H),
1.20 (s, 6H).
229 8 7.20 (m, SH), 4.66 (m, 1H), 2.64 (t, 2H), 2.13 (s, 3H),
1.59 (m, 2H), 1.35 (m, 2H), 1.23 (m, 6H),
0.94 (t, 3H).
230 8 7.40-7.13 (m, 8H), 4.68 (m, 1H), 2.69 (q, 2H), 2.14
(s, 3H), 1.26 (m, 9H).
232 8 7.37 (m, 3H), 7.20-7.30 (m, 2H), 4.68 (s, 2H), 4.61
(m, 1H), 2.61 (s, 3H), 2.41 (s, 3H), 1.20 (d,
6H).
233 8 7.37 (dd, 1H), 6.92 (dd, 1H), 4.69 (s, 2H), 4.61 (m,
1H), 2.61 (s, 3H), 2.41 (s, 3H), 1.21 (d, 6H).
236 8 7.28 (m, 8H), 4.53 (m, 1H), 2.33 (s, 3H), 2.20 (s, 1.SH),
2.07 (s, 1.SH), 1.44 (d, 3H), 1.16 (d, 3H).
238 8 7.40 (m, 3H), 5.05 (m, 1H), 4.60 (m, 1H), 1.80 (d, 3H),
1.20 (m, 6H).
241 8 7.37 (d, 2H), 7.19 (d, 2H), 4.61 (m, 1H), 2.65 (m, 1H),
1.119 (d, 6H), 0.97 (m, 4H).
248 8 7.40 (m, 2H), 7.05 (m, 2H), 4.80 (q, 1H), 4.25 (q, 2H),
3.55 (q, 2H), 1.43 (d, 3H), 1.30 (m, 12H).
251 8 7.23 (m, 2H), 7.11 (m, 2H), 4.65 (m, 1H), 3.34 (d, 2H),
1.22 (m, 7H), 0.55 (m, 2H), 0.35 (m, 2H).
252 8 7.22 (m, 2H), 7.08 (m, 2H), 4.65 (m, 1H), 4.25 (s, 2H),
2.48 (q, 2H), 1.19 (d, 6H), 1.1 (t, 3H).
253 8 7.22 (m, 2H), 7.08 (m, 2H), 4.65 (m, 1H), 3.4 (m, 4H),
1.9-1.19 (m, 34H), 0.88 (m, 7H).
254 8 7.23 (m, 2H), 7.09 (m, 2H), 4.65 (m, 1H), 4.22 (m, 2H),
2.13 (m.2H), 1.45 (m, 2H), 1.29 (m, 4H), 1
0.88 (m, 3H).
256 8 7.2 (m, 2H), 7.04 (m, 2H), 4.61 (m, 3H), 3.88 (s, 2H),
1.43 (s, 2H), 0.04 (m, 9H).
257 S 7.23 (m, 2H), 7.1 (m, 2H), 4.65 (m, 1H), 3.46 (m, 3H),
1.67-0.9 (m, 18H).
258 b 7.23 (m, 2H), 7.08 (m, 2H), 4.98 (s, 2H), 4.65 (m, 1H),
3.71 (m, 2H), 3.45 (m, 2H), 3.28 (s, 3H),
1.2 (d, 6H).
260 8 7.75 (d, 2H), 7.6 (t, 1H), 7.45 (t, 2H), 7.2 (m, 2H),
7.05 (m, 2H), 5.38 (q, 1H), 4.65 (m, 1H), 1.73
(d, 3H), 1.19 (d, 6H).
262 8 7.23 (m, 2H), 7.08 (m, 2H), 5.17 (m, 1H), 5.02 (m, 1H),
4.65 (m, 1H), 4.06 (d, 2H), 2.02 (m, 4H), i
1.65 (s, 3H), 1.57 (s, 3H), 1.19 (d, 6H).
263 8 7.22 (m, 2H), 7.1 (m, 2H), 6.75 (m, 1H), 6.92 (m, 1H),
4.65 (m, 1H), 4.22 (m, 2H), 3.74 (s, 3H),
1.2 (d, 6H).
264 8 7.22 (m, 2H), 7.08 (m, 2H), 4.65 (m, 1H), 4.07 (s, 2H),
3.38 (m, 4H), 1.24-1.14 (m, 12H).
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265 8 7.23 (m, 2H), 7.08 (m, 2H), 4.65 (m, 1H), 4.09 (s, 2H),
1.43 (s, 9H), 1.19 (d, 6H).
266 8,7.21 (m, 2H), 7.08 (m, 2H), 4.65 (m, 1H), 3.66 (s, 3H),
3.55 (t, 2H), 2.33 (t, 2H), 1.96 (m, 2H), 1.2
267 8 8.53 (m, 1H), 7.76 (m, 1H), 7.25 (m, 6H), 7.08 (t, 2H),
4.76 (s, 2H), 4.66 (m, 1H), 1.19 (d, 6H).
274 8 3.90 (m, 1H), 3.40 (q, 2H), 2.97 (s, 6H), 1.50 (bm,
15H).
275 S 3.90 (m, 1H), 3.45 (m, 4H), 1.70 (bm, lOH), 1.00 (s,
9H),
277 8 7.30 (m, 1H), 6.90 (m, 2H), 4.70 (m, 1H), 3.20 (s, 2H),
1.20 (m, 6H), 0.90 (s, 9H).
279 8 7.4 (m, 2H), 7.05 (m, 2H), 5.80 (m, 1H), 5.30 (m, 1H),
5.25 (m, 1H), 4.80 (q, 1H), 4.25 (m, 2H),
4.6 (m, 2H), 1.42 (d, 3H), 1.30 (m, 6H).
280 8 7.4 (m, 2H), 7.05 (m, 2H), 4.80 (q, 1H), 4.25 (q, 2H),
3.75 (m, 1H), 1.00-2.00 (m, 19H).
283 b 7.40-7.20 (m, SH), 4.6 (m, 1H), 4.10 (m, 1H), 1.80 (m,
8H), 1.20 (d, 6H).
284 8 7.40 (m, 1H), 6.80 (m, 2H), 4.6 (m, 1H), 4.10 (m, 1H),
1.80 (m, 8H), 1.20 (d, 6H).
285 8 7.23 (m, 2H), 7.08 (m, 2H), 5.5 (t, 1H), 4.65 (m, 1H),
4.2 (d, 2H), 2.12 (s, 3H), 1.2 (d, 6H).
286 8 7.23 (m, 2H), 7.11 (m, 2H), 5.8 (m, 1H), 5.4 (m, 1H),
4.65 (m, 1H), 4.0 (d, 2H), 2.05 (m, 2H), 1.2
(d, 6H), 0.96 (t, 3H).
287 8 7.21 (m, 2H), 7.09 (m, 2H), 4.65 (m, 1H), 4.54 (t, 1H),
4.38 (t, 1H), 3.65 (t, 2H), 2.05 (m, 2H), 1.2
(d, 6H).
288 8 7.21 (m, 2H), 7.08 (m, 2H), 5.2 (m, 1H), 4.65 (m, 1H),
4.05 (d, 2H), 1.73 (d, 6H), 1.2 (d, 6H).
289 8 7.23 (m, 2H), 7.09 (m, 2H), 4.65 (m, 1H), 4.52 (t, 1H),
4.36 (t, 1H), 3.53 (t, 2H), 1.8-1.6 (m, 4H),
1.2 (d, 6H).
290 8 7.23 (m, 2H), 7.08 (m, 2H), 4.65 (m, 1H), 3.46 (t, 2H),
1.6 (m, 2H), 1.3 (m, 4H), 1.19 (d, 6H),
0.87 (t, 3H).
291 8 7.22 (m, 2H), 7.09 (m, 2H), 5.72 (m, 1H), 4.99 (m, 2H),
4.65 (m, 1H), 3.48 (t, 2H), 2.05 (q, 2H), 1.
1.2 (d, 6H).
292 b 7.38-7.35 (m, 2H), 7.21-7.18 (m, 2H), 4.65 (m, 1H),
2.93 (s, 2H), 1.2 (d, 6H), 0.08 (s, 9H).
293 8 7.22 (m, 2H), 7.09 (m, 2H), 4.89 (s, 2H), 4.65 (m, 1H),
3.39 (s, 3H), 1.2 (d, 6H).
294 8 7.23 (m, 2H), 7.08 (m, 2H), 4.65 (m, 1H), 2.93 (s, 2H),
1.2 (d, 6H), 0.08 (s, 9H).
295 8 7.23 (m, 2H), 7.09 (m, 2H), 4.92 (s, 2H), 4.65 (m, 1H),
3.58 (q, 2H), 1.2 (m, 9H).
296 8 8.59 (s, 1H), 8.51 (s, 2H), 4.7 (m, 1H), 4.2-4.1 (m,
1H), 1.4-1.3 (m, 12H).
297 8 3.49 (m, 1H), 2.77 (m, 1H), 1.25 (, 6H), 1.05 (m, 4H).
298 S 3.9 (m, 1H), 3.41 (q, 2H), 2.79 (m, 1H), 2-1 (m, 17H).
302 8 7.4 (m, 2H), 7.1 (m, 2H), 4.8 (m, 1H), 4.3 (m, 3H),
1.5-1.2 (m, 12H).
303 8 7.4 (m, 4H), 7.2-7.3 (m, 1H), 7.1-7.2 (m, 2H), 4.7-4.8
(m, 1H), 2.306 (s, 3H), 1.3-1.4 (m, 9H), 1.2
(m, 3H), 1.1 (m, 3H).
304 8 7.40 (t, 1H), 7.26 (m, 1H), 7.15 (d, 2H), 7.10 (m, 2H),
4.70 (m, 1H), 2.38 (q, 4H), 1.20 (d, 6H),
1.10 (t, 6H).
308 8 3.95 (m, 1H), 3.40 (m, 1H), 2.10 (m, 1H), 1.80 ( (m,
3H), 1.70-1.20 (m, 6H).
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309 8 4.28 (m, 1H), 3.80 (m, 1H), 3.40 (m, 2H), 1.8 (m, 2H)1.25
(d, 6H), 1.20 (t, 3H).
312 8 7.40 (m, 1H), 6.42 (s, 1H), 6.40 (s, 1H), 4.74 (s, 2H),
3.84 (M, 1H), 3.40 (m, 2H), 1.80 (4H), 1.20
(t, 3H).
317 $ 7.20 (m, 2H), 7.10 (m, 2H), 4.70 (m, 1H), 3.50 (d, 2H),
3.30 (s, 6H), 1.20 (d, 6H).
323 8 7.22 (m, 2H), 7.07 (m, 2H), 4.6 (m, 1H), 3.55 (t, 2H),
2.26 (t, 2H), 2.11 (s, 6H), 1.8 (t, 2H), 1.2 (d,
6H)
325 8 7. 4 (m, 2H), 7.3 (m, 2H), 5.9-5.7 (m, 1H), 5.3-5.2
(m, 2H), 4.1 (d, 2H), 3.7 (q, 1H), 1.3 (d, 3H),
0.7-0.4 (m, 4H), 0.3 (m, 1H).
331 8 7.4 (m, 2H), 7.30 (t, 1H), 7.05 (t, 2H), 6.95 (d, 1H),
6.90 (d, 1H), 4.80 (q, 1H), 4.25 (q, 2H), 3.75
(s, 3H), 2.12 (s, 3H), 1.45 (s, 3H), 1.30 (t, 6H).
335 8 8.18 (d, 1H), 8.08 (d, 1H), 7.82 (d, 1H), 7.62-7.44
(m, 6H), 7.20 (m, 1H), 4.60 (m, 1H), 1.20 (br. s,
6H) (In DMSO).
336 8 8.18-8.00 (m, 2H), 7.60-7.43 (m. 8H), 4.62 (m, 1H),
2.24 (s, 3H), 1.20 (m, 6H) (in DMSO).
337 b 8.14-8.00 (m, 2H), 7.60-7.20 (m, 7H), 4.62 (m, 1H),
2.20 (s, 3H), 1.20 (s, 6H) (in DMSO).
338 8 8.12-8.00 (m, 2H), 7.60-7.22 (m, 8H), 4.60 (m, 1H),
2.24 (s, 3H), 1.19 (d, 6H) (in DMSO).
344 8 8.10-8.00 (m, 2H), 7.60-7.22 (m, 9H), 4.62 (m, 1H),
2.22 (s, 3H), 1.20 (m, 6H) (in DMSO).
345 8 7.40-7.20 (m, 4H), 5.60 (m, 1H), 5.02 (m, 1H), 4.60
(m, 1H), 4.00 (m, 1H), 3.60 (m, 1H), 3.40 (m,
1H), 1.20 (d, 6H).
352 8 7.30 (m, 1H), 6.90 (m, 2H), 4.65 (m, 1H), 4.20 (m, 1H),
3.75 (t, 1H), 3.40 (q, 1H), 3.20 (s, 3H),
1.30 (d, 3H), 1.20 (m, 6H).
354 8
355 8 7.30 (m, 1H), 6.90 (m, 2H), 4.70 (m, 1H), 3.60 (m, 1H),
2.20 (m, 1H), 1.35 (s, 3H), 1.20 (m, 6H),
0.90 (d, 3H), 0.80 (d, 3H).
356 S 7.40 (m, 3H), 7.28 (m, 2H), 4.70 (m, 1H), 3.60 (m, 1H),
2.20 (m, 1H), 1.35 (s, 3H), 1.20 (d, 6H),
0.90 (d, 3H), 0.80 (d, 3H).
358 8 7.20 (m, 2H), 7.10 (m, 2H), 4.70 (m, 1H), 1.90 (m, 2H),
1.70 (m, 2H), 1.20 (d, 6H), 0.80 (t, 6H).
359 8 7.2-7.4 (m, 2H), 7.15 (m, 2H), 7.0-7.1 (t, 3H), 4.7-4.8
(m, 1H), 2.308 (s, 3H), 1.3-1.4 (m, 12H),
1.16 (s, 3H).
361 8 7.37 (d, 2H), 7.18 (d, 2H), 4.64 (m, 1H), 1,39 (s, 3H),
1.19 (d, 6H), 1.02 (m, 2H), 0.86 (m, 2H).
362 8 7.24 (d, 2H), 7.18 (d, 2H), 4.64 (m, 1H), 1,39 (s, 3H),
1.19 (d, 6H), 1.02 (m, 2H), 0.86 (m, 2H).
363 S 7.37 (d, 1H), 6.92 (m, 2H), 4.64 (m, 1H), 1,39 (s, 3H),
1.19 (d, 6H), 1.02 (m, 2H), 0.86 (m, 2H).
364 8 7.40 (m, 3H), 7.28 (m, 2H), 4.70 (m, 1H), 3.60 (m, 1H),
1.90 (m, 2H), 1.70 (m, 2H), 1.20 (d, 6H),
0.80 (d, 6H).
365 8 7.4 (m, 2H), 7.2 (m, 2H), 4.8 (m, 1H), 4.2 (m, 2H),
3.0 (s, 3H), 1.4 (d, 3H), 1.3 (t, 3H).
366 8 8.61 (m, 2H), 7.70 (br d, 1H), 7.27 (m, 3H), 7.07 (t,
1H), 4.73 (m, 1H), 4.62 (s, 2H), 1.19 (d, 6H).
367 b 7.23 (m, 2H), 7.11 (m, 2H), 4.67 (m, 1H), 4.2 (m, 1H),
3.93 (m, 1.H), 3.6 (m, 1H), 1.48 (d, 3H),
1.18 (d, 6H).
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369 8 7.37 (q, 1H), 7.19 (d, 2H), 4.64 (m, 1H), 2.31 (b, 1H),
1.4-0.77 (m, 12H).
370 8 7.39 (m, 3H), 7.24 (m, 2H), 4.64 (m, 1H), 2.28 (m, 1H),
1.3-1 (m, 11H), 0.78 (m, 1H).
372 8 7.37 (q, 1H), 6.92 (m, 2H), 4.64 (m, 1H), 2.31 (m, 1H),
1.4-1.0 (m, 11H), 0.78 (m, 1H).
379 b 7.38 (m, 3H), 7.22 (m, 2H), 4.83 (s, 2H), 4.62 (m, 1H),
4.46 (q, 2H), 1.41 (t, 3H), 1.21 (d, 6H).
381 8 7.22 (m, 3H), 7.06 (m, 3H), 4.85 (s, 2H), 4.63 (m, 1H),
4.48 (m, 2H), 1.42 (t, 3H), 1.19 (d, 6H.
387 8 7.3 (m, 2H), 7.1 (m, 2H), 4.93 (m, 1H), 4.65 (m, 1H),
1.8 (d, 3H), 1.2 (d, 6H).
389 8 7.23 (m, 2H), 7.08 (m, 2H), 4.65 (m, 1H), 3.46 (t, 2H),
1.6 (m, 2H), 1.26 (m, 6H), 1.2 (d, 6H),
0.86 (t, 3H).
394 8 7.28 (m, 1H), 6.91 (m, 2H), 4.65 (m, 1H), 3.29 (d, 2H),
2.11 (m, 1H), 1.21 (b, 6H), 0.87 (D, h
399 8 7.24 (m, 2H), 7.1 (m, 2H), 4.64 (m, 1H), 3.77 (m, 2H),
2.45 (m, 2H), 1.21 (d, 6H).
400 8 7.21 (m, 2H), 7.09 (m, 2H), 4.65 (m, 1H), 4.47 (q, 1H),
2.19 (s, 3H), 1.67 (d, 3H), 1.2 (d, 6H).
401 8 7.05-7.24 (m, 4H), 5.37-5.44 (m, 1H), 4.58-4.67 (m,
1H), 2.33 (s, 3H), 1.78 (d, 3H), 1.19 (d, 6H).
408 S 7.27 (m, 1H), 6.89 (m, 2H), 4.62 (m, 1H), 4.2 (m, 1H),
3.98 (m, 1H), 3.6 (m, 1H), 1.45 (d, 3H),
1.21 (d, 6H).
412 8 7.20-7.10 (m, 4H), 5.80 (m, 1H), 5.40 (m, 1H), 4.60
(m, 1H), 4.05 (d, 1H), 4.00 (d, 1H), 1.70 (m,
2H), 1.20 (d, 6H).
413 b 7.20 (m, 2H), 7.10 (m, 2H), 6.00 (m, 1H), 5.20 (m, 2H),
4.60 (m, 2H), 1.50 (d, 3H), 1.20 (d, 6H).
414 8 7.36 (m, 2H), 7.19 (m, 2H), 6.02 (m, 2H), 5.69 (m, 1H),
4.64 (septet, J = 6.8 Hz, 1H), 2.97 (s, 2H),
1.20 (d, J = 6.8 Hz, 8H), 0.17 (s, 6H).
417 b 7.38 (m, 2H), 7.17 ( m, 2H), 4.65 (m, 1H), 3.29 (d,
2H), 2.01 (m, 1H), 1.21 (d, 6H), 0.88 (d, 6H).
418 8 7.38 (m, 2H), 7.25 (m, 2H), 4.75 (s, 1H), 4.63 (m, 1H),
4.6 (m, 1H), 3.57 (t, 2H), 2.31 (t, 2H), 1.71
(s, 3H), 1.2 (d, 6H).
419 8 7.38 (m, 2H), 7.25 (m , 2H), 4.62 (m, 1H), 3.68 (t,
2H), 2.73 (t, 2H), 2.06 (s, 3H), 1.2 (d, 6H).
420 8 7.38 (m, 3H), 7.25 (m , 2H), 4.53 (d, 2H), 4.31 (d,
2H), 3.67 (s, 3H), 1.27 (s, 3H), 1.2 (d, 6H).
424 8
425 b 7.23 (m, 2H), 7.08 (m, 2H), 6.01 (m, 2H), 5.70 (dd,
J = 16.5 Hz, J = 7.3 Hz, 1H), 4.65 (septet, J =
6.8 Hz, 1 H), 2.97 (s, 2H), 1.19 (d, J = 6.8 Hz, 6H),
0.17 (s, 6H).
426 b 7.23 (m, 2H), 7.05 (m, 2H), 5.69 (m, 1H), 5.29 (s, 2H),
4.85 (m, 2H), 4.65 (septet, J = 6.8 Hz, 1H),
2.95 (s, 2H), 1.58 (d, J = 8.1 Hz, 2H), 1.19 (d, J = 6.8
Hz, 6H).
427 8 5.82 (s, 1H), 4.25 (m, 1H), 4.20 (s, 1H), 4.00 (t, 2H),
2.25 (s, 1H), 1.20 (m, 6H).
428 8 5.78 (s, 1H), 4.25 (m, 1H), 4.00 (m, 1H), 2.25 (m, 1H),
2.20 (m, 4H), 1.20 (d, 6H).
429 8 4.00 (m, 1H), 3.50 (m, 2H), 3.00 (m, 1H), 2.20 (m, 2H),
1.80 (m, 4H), 1.20 (t, 3H).
432 8 7.35 (m, 2H), 7.0 (m, 1H), 4.9 (m, 1H), 4.6 (m, 1H),
1.8 (d, 3H), 1.2 (br, 6H).
435 8 7.4-7.2 (m, SH), 4.9 (m, 1H), 4.62 (m, 1H), 1.7 (d,
3H), 1.2 (d, 6H).
441 8 7.3 (m, 3H), 7.2 (m, 3H), 5.0 (m, 1H), 4.6 (m, 1H),
3.2 (s, 3H), 1.6 (d, 3H), 1.1 (d, 6H).
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442 8 7.37 (m, 3H), 7.20 (m, 2H), 5.40 (q, 1H), 4.61 (m,
lI-17, 2, 62 (s, 3H), 2.30 (s, 3H), 1.76 (d, 3H),
1.20 (d, 6H).
443 8 7.30 (m, 1H), 6.90 (t, 2H), 5.40 (q, 1H), 4.60 (m,
1H), 2.62 (s, 3H), 2.32 (s, 3H), 1.77 (d, 3H),
1.20 (m, 6H).
446 S 7.2 (m, 2H), 7.1 (m, 2H), 5.1 (m, 1H), 4.7 (m, 1H),
3.9 (m, 1H), 3.7 (m, 1H), 3.4 (s, 3H), 3.3 (s,
3H), 1.2 (s, 6H).
447 8 7.4 (m, 3H), 7.3 (m, 2H), 4.6 (m, 1H), 4.1 (m, 4H),
3.8 (d, 2H), 1.2 (m, 12H).
448 8 7.4 (m, 3H), 7.3 (m, 2H), 4.6 (m, 1H), 4.3 (m, 1H),
4.1 (m, 4H), 1.6 (m, 6H), 1.2 (m, 12H).
452 8 7.2 (m, 2H), 7.1 (m, 2H), 6.1-5.2 (m, 3H), 4.7 (m,
1H), 3.6 (m, 1H), 3.4 (s, 3H), 3.4 (s, 3H), 1.2 (d,
6H).
453 8 7.21 (m, 2H), 7.08 (m, 2H), 4.6 (m, 1H), 3.99 (t, 2H),
3.36 (t, 2H), 2.97 (s, 3H), 1.18 (d, 6H).
454 8 7.39 (m, 3H), 7.26 (m, 2H), 5.8 (m, 1H), 5.38 (m, 1H),
4.68 (m, 1H), 3.99 (d, 2H), 2.0 (m, 2H),
1.2 (d, 6H), 0.95 (t, 3H).
455 b 7.39 (m, 3H), 7.26 (m, 2H), 6.0 (m, 1H), 5.2 (dd, 2H),
4.65 (m, 1H), 4.2 (m, 1H), 1.9 (m, 2H),
1.21 (d, 6H), 0.83 (t, 3H).
456 S 7.39 (m, 2H), 7.20 (m, 2H), 4.65 (m, 1H), 4.2 (m, 1H),
3.91 (m, 1H), 3.6 (dd, 1H), 1.46 (d, 3H),
1.21 (d, 6H).
457 8 7.4 (m, 3H), 7.2 (m, 2H), 5.0 (s, 2H), 4.5-4.0 (br,
1H), 1.6 (m, 1H), 1.2 (d, 6H).
458 8 7.3 (m, 2H), 7.1 (m, 2H), 5.1 (m, 1H), 4.7 (m, 1H),
4.1 (m, 1H), 3.8 (m, 1H), 3.4 (s, 3H), 1.2 (d;
6H).
461 S 7.27 (m, 2H), 7.11 (m, 2H), 4.68 (m, 1H), 3.46 (t,
2H), 1.64 (m, 2H), 1.22 (d, 6H), 0.44 (m, 2H),
0.00 (s, 9H).
463 8 7.3-7.4 (q, 1H), 6.8-7.0 (m, 2H), 4.6-4.7 (m, 2H),
3.73 (s, 3H), 1.6 (d, 3H), 1.2 (d, 6H).
464 8 7.4 (m, 3H), 7.2 (m, 2H), 4.6-4.7 (m, 2H), 3.727 (s,
3H), 1.6 (d, 6H), 1.3 (d, 3H).
465 8 7.3-7.4 (m, 1H), 6.8-7.0 (m, 2H), 4.6-4.7 (m, 1H),
4.1-4.3 (m, 3H), 3.5-3.9 (m, 1H), 3.0-3.3 (m,
1H), 2.2-2.5 (m, 1H), 1.2 (m, 12H).
467 8 7.39 (m, 2H), 7.22 (m, 2H), 4.93 (s, 2H), 4.66 (septet,
J = 6.8 Hz, 1H), 3.62 (apparent t, J = 8.3
Hz, 2H), 1.22 (d, J = 6.8 Hz, 6H), 0.93 (apparent t,
J = 8.3 Hz, 2H), 0.00 (s, 9H).
472 8 7.35 (m, 1H), 7.00 (m, 2H), 4.70 (m, 1H), 4.00 (m,
1H), 3.38 (s, 3H), 3.23 (s, 3H), 1.35 (d, 3H),
1.20 (m, 6H).
478 S 1.18 (d, 6H), 1.68 (d, 3H), 2.95 (s, 3H) 2.98 (s, 3H),
4.64 (m, 1H), 4.83 (q, 1H) 7.05 (m, 2H), 7.22
(m, 2H).
479 8 1.20 (d, 6H), 1.66 (d, 3H), 2.94 (s, 3H), 2.96 (s,
3H), 4.65 (m, 3H), 4.82 (q, 1H), 7.21 (m, 2H),
7.38 (m, 2H).
481 S 1.20 (m, 6H), 1.68 (d, 3H), 2.94 (s, 3H), 2.99 (s,
3H), 4.64 (m, 1H), 4.82 (q, 1H), 6.89 (m, 2H),
7.33 (m, 1H).
485 8 7.39 (m, 3H), 7.24 (m, 2H), 4.64 (m, 1H), 4.3 (s, 2H),
2.64 (m, 1H) 1.21 (d, 6H), 1.16 (d, 6H).
486 8 7.34 (q, 1H), 6.93 (m, 2H), 4.64 (m, 1H), 4.3 (s, 2H),
2.64 (m, 1H), 1.22 (b, 6H), 1.16 (d, 6H).
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487 8 7.37 (d, 2H), 7.18 ( d, 2H), 4.64 (m, 1H), 2.65 (m,
1H), 1.19 (m, 12H).
488 8 7.20 (m, 2H), 7.09 (m, 2H), 4.64 (m, 1H), 4.43 (s, 2H),
1.92 ( m, 1H), 1.19 (m, 8H), 1.04 (m, 2H).
490 8 7.34 (m, 1H), 6.95 (m, 2H), 4.64 (m, 1H), 4.42 (s, 2H),
1.92 (m, 1H), 1.22 (m, 8H), 1.03 (m, 2H).
491 8 9.53 (s, 1H), 7.24 (m, 2H), 7.1 (m, 2H), 4.64 (m. 1H),
4.35 (s, 2H), 1.2 (b, 6H).
492 8 7.3-7.2 (m, 2H), 7.1 (m, 2H), 6.1 (bs, 1H), 4.7 (m,
1H), 4.14 (s, 2H), 3.7-3.6 (m, 4H), 1.20 (d, 6H).
493 8 7.3-7.2 (m, 2H), 7.1 (m, 2H), 5.9 (bs, 1H), 4.7-4.6
(m, 1H), 4.09 (s, 2H), 3.6-3.5 (t, 2H), 3.5 (dt,
2H), 2.0 (m, 2H), 1.20 (d, 6H).
494 8 7.4 (m, 3H), 7.3-7.2 (m, 2H), 4.7 (m, 1H), 4.14 (t,
2H), 4.02 (s, 2H), 3.3 (t, 2H), 1.9-1.8 (m, 2H),
1.21 (d, 6H).
495 8 7.4 (m, 3H), 7.3-7.2 (m, 2H), 4.7-4.6 (m, 1H), 4.3 (t,
2H), 4.24 (s, 2H), 3.9-3.8 (t, 2H), 1.21 (d,
6H).
496 8 7.4-7.3 (m, 3H), 7.2-7.1 (m, 2H), 5.6 (bs, 1H), 4.7-4.6
(m, 1H), 3.9 (s, 2H), 2.0 (bs, 2H), 1.9 (bs,
2H), 1.6-1.4 (m, 4H), 1.2 (d, 6H).
497 8 7.3 (m, 3H), 7.2 (m, 2H), 5.8 (s, 1H), 4.7-4.6 (m, 1H),
3.94 (s, 2H), 2.7 (m, 2H), 2.4 (m, 2H), 2.2
(b, 2H), 1.2 (d, 6H).
498 8 8.7-8.6 (bs, 1H), 8.5 (bs, 1H), 7.7 (m, 1H), 7.4-7.2
(m, 6H), 5.5 (s, 1H), 5.3 (s, 1H), 4.7-4.6 (m,
1H), 4.45 (s, 2H), 1.2 (d, 6H).
500 S 7.3 (m, 1H), 6.9 (m, 2H), 4.64 (m, 1H), 4.48 (d of t,
2H), 3.65 (t, 2H), 2.42 (m, 2H), 1.2 (m, 6H).
501 8 7.3 (m, 1H), 6.9 (m, 2H), 4.87 (m, 1H), 4.64 (m, 1H),
3.86 (m, 2H), 3.77 (m, 2H), 3.64 (t, 2H),
2.05 (m, 2H), 1.2 (m, 6H).
502 S 7.4 (m, 1H), 6.9 (m, 2H), 4.64 (m, 1H), 4.57 (m, 1H),
3.97 (m.2H), 3.63 (m, 4H), 1.97 (m, 3H),
1.2 (m, 7H).
503 S 7.3 (m, 1H), 6.9 (m, 2H), 4.88 (s, 2H), 4.64 (m, 1H),
3.93 (s, 3H), 1.2 (m, 6H).
504 b 7.4 (m, 1H), 6.9 (m, 2H), 4.92 (s, 2H), 4.65 (m, 1H),
3.59 (q, 2H), 1.2 (m, 9H).
505 8 7.4 (m, 1H), 6.9 (m, 2H), 4.97 (s, 2H), 4.63 (m, 1H),
3.72 (m, 2H), 3.45 (m, 2H), 3.30 (s, 3H), 1.2
(
506 8 7.4 (m, 1H), 6.9 (m, 2H), 4.63 (m, 1H), 4.05 (m, ZH),
3.51 (m, 2H), 2.04 (s, 3H), 1.67 (m, 4H), 1.2
(m, 6H).
507 8 7.35 (m, 2H), 6.92 (m, 2H), 4.64 (m, 1H), 3.7 (t, 2H),
2.65 (m, 2H), 1.23 (br s, 6H).
508 8 7.3 (m, 4H), 7.1 (m, 2H), 6.9 (m, 2H), 4.62 (m, 1H),
3.69 (m, 2H), 2.92 (m, 2H), 1.2 (m, 6H)
509 S 7.3 (m, 1H), 6.9 (m, 2H), 4.65 (m, 1H), 3.33 (m, 2H),
1.2 (m, 7H), 0.54 (m, 2H), 0.33 (m, 2H)
510 8 7.3 (m, 1H), 6.9 (m, 2H), 4.63 (m, 1H), 4.37 (s, 2H),
2.43 (s, 3H), 2.24 (s, 3H), 1.2 (m, 6H).
511 S 7.75 (d, 2H), 7.6 (t, 1H), 7.45 (t, 2H), 7.3 (m, 1H),
6.89 (m, 2H), 5.37 (q, 1H), 4.65 (m, 1H), 1.72
(d, 3H), 1.2 (br s, 6H).
512 8 7.3 (m, 1H), 6.9 (m, 2H), 4.65 (m, 1H), 4.23 (s, 2H),
3.36 (q, 2H), 3.26 (q, 2H), 1.21 (m, 9H), 1.11
(t, 3H).
513 8 7.35 (m, 1H), 6.92 (m, 2H), 4.65 (m, 1H), 3.66 (s, 3H),
3.53 (t, 2H), 2.31 (t, 2H), 1.96 (m, 2H),
1.22 (br s, 6H).
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514 S .35 (m, 1H), 6.92 (m, 2H), 5.55 (t, 1H), 4.65 (m, 1H),
4.2 (d, 2H), 2.12 (s, 3H), 1.21 (br s, 6H).
(3:1 cis/trans mix.)
515 8 7.35 (m, 1 H), 6.92 (m, 2H), 5.2 (t, 1 H), 4.65 (m,
1 H), 4.04 (d, 2H), 1.72 (m, 6H), 1.21 (br s, 6H).
516 8 7.35 (m, 1H), 6.92 (m, 2H), 5.73 (m, 1H), 5.0 (m, 2H),
4.65 (m, 1H), 3.48 (t, 2H), 2.04 (q, 2H), 1.7
1.22 (br s, 6H).
517 8 7.32 (m, 1H), 6.91 (m, 2H), 4.65 (m, 1H), 4.48 (q, 1H),
2.19 (s, 3H), 1.65 (d, 3H), 1.22 (br s, 6H).
518 8 7.35 (m, 1H), 6.89 (m, 2H), 4.65 (m, 1H), 2.93 (s, ZH),
1.21 (br s, 6H), 0.08 (m, 9H).
519 8 7.37 (m, 1H), 6.92 (m, 2H), 5.1 (s, 1H), 4.87 (s, 2H),
4.65 (m, 1H), 4.13 (q, 2H), 3.78 (q, 2H), 1.23
520 S 7.3 (m, 6H), 6.9 (m, 2H), 4.98 (s, 2H), 4.6 (m, 3H),
1.21 (br s, 6H).
521 S 7.35 (m, 1H), 6.9 (m, 2H), 4.64 (m, 1H), 3.5 (d, 2H),
2.65 (m, 1H), 2.0-1.7 (m, 6H), 1.21 (br s,
6H).
522 8 7.35 (m, 1H), 6.92 (m, 2H), 4.65 (m, 1H), 4.52 (t, 1H),
4.36 (t, 1H), 3.53 (t, 2H), 1.85-1.6 (m, 4H),
1.22 (br s, 6H).
523 S 7.35 (m, 1H), 6.9 (m, 2H), 5.8 (m, 1H), 5.4 (m, 1H),
4.65 (m, 1H), 4.0 (d, 2H), 2.03 (m, 2H), 1.21
(br s, 6H), 0.94 (t, 3H)
524 8 7.32 (m, 1H), 6.92 (m, 2H), 4.65 (m, 1H), 4.24 (s, 2H),
2.47 (q, 2H), 1.21 (br s, 6H), 1.1 (t, 3H).
525 8 7.33 (m, 1H), 6.93 (m, 2H), 4.65 (m, 1H), 3.75 (t, 2H),
2.48 (m, 2H), 1.22 (br s, 6H).
526 8 7.33 (m, 1H), 6.93 (m, 2H), 4.65 (m, 1H), 3.55 (t, 2H),
2.1 (m, 2H), 1.92 (m, 2H), 1.23 (br s, 6H)
527 8 7.39 (m, 2H), 7.22 (m, 2H), 4.93 (s, 2H), 4.66 (septet,
J = 6.8 Hz, 1H), 3.62 (apparent t, J = 8.3
Hz, 2H), 1.22 (d, J = 6.8 Hz, 6H), 0.93 (apparent t, J
= 8.3 Hz, 2H), 0.00 (s, 9H).
528 8 7.3 (d, 2H), 7.1 (d, 2H), 4.6-4.7 (m, 1H), 3.5 (t, 2H),
1.6 (m, 2H), 1.3 (m, 4H), 1.1 (d, 6H), 0.875
(t, 3H).
529 8 7.3 (d, 2H), 7.1 (d, 2H), 4.6-4.7 (m, 1H), 3.4 (t, 2H),
1.6 (m, 2H), 1.26 (brd s, 6H), 1.1 (d, 6H),
0.865 (t, 3H).
530 8 7.3 (d, 2H), 7.1 (d, 2H), 4.6-4.7 (m, 1H), 4.5 (t, 1H),
4.4 (t, 1H), 3.6 (t, 2H), 1.9-2.1 (m, 2H), 1.2
(d, 6H).
531 8 7.3 (d, 2H), 7.1 (d, 2H), 4.875 (m, 1H), 4.6-4.7 (m,
1H), 3.7-3.9 (m, 4H), 3.648 (t, 2H), 2.046 (m,
2H), 1.1 (d, 6H).
532 8 7.3 (d, 2H), 7.1 (d, 2H), 4.6-4.7 (m, 1H), 4.561 (m,
1H), 3.9-4.0 (m, 2H), 3.6 (m, 4H), 1.9-2.0 (m,
3H), 1.3 (brd s, 1H), 1.1 (d, 6H).
533 8 7.3 (d, 2H), 7.1 (d, 2H), 4.886 (s, 2H), 4.6-4.7 (m,
1H), 3.394 (s, 3H), 1.2 (d, 6H).
534 S 7.4 (d, 2H), 7.2 (d, 2H), 4.922 (s, 2H), 4.6-4.7 (m,
1H), 3.6 (q, 2H), 1.1-1.2 (m, 9H).
535 8 7.3 (d, 2H), 7.1 (d, 2H), 4.977 (s, 2H), 4.6-4.7 (m,
1H), 3.708 (m, 2H), 3.470 (m, 2H), 3.277 (s,
3H), 1.2 (d, 6H).
536 8 7.3 (d, 2H), 7.1 (d, 2H), 4.6-4.7 (m, 1H), 4.056 (t,
2H), 3.508 (t, 2H), 2.039 (s, 3H), 1.6-1.8 (m,
4H), 1.2 (d, 6H).
537 b 7.3 (d, 2H), 7.1 (d, 2H), 4.6-4.7 (m, 1H), 3.7 (t, 2H),
2.6-2.8 (m, 2H), 1.2 (d, 6H).
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538 b 7.3 (d, 2H), 7.238 (m, 2H), 7.166 (m, 1H), 7.0-7.1 (m,
4H), 4.6-4.7 (m, 1H), 3.7 (t, 2H), 2.9 (t,
2H), 1.2 (d, 6H).
539 b 7.3 (d, 2H), 7.1 (d, 2H), 4.6-4.7 (m, 1H), 3.3 (d, 2H),
1.2 (d, 6H), 1.1-1.2 (m, 1H), 0.56 (q, 2H),
0.3 (q, 2H).
540 8 7.3 (d, 2H), 7.1 (d, 2H), 4.6-4.7 (m, 1H), 4.369 (s,
2H), 2.436 (s, 3H), 2.245 (s, 3H), 1.1 (d, 6H).
541 8 7.77 (d, 2H), 7.6 (t, 1H), 7.4 (t, 2H), 7.3 (d, 2H),
7.1 (d, 2H), 5.3-5.4 (q, 1H), 4.6-4.7 (m, iH), 1.7
(d, 3H), 1.1 (d, 6H).
542 8 7.3 (d, 2H), 7.1 (d, 2H), 4.6-4.7 (m, 1H), 4.230 (s,
2H), 3.4 (q, 2H), 3.2-3.2 (q, 2H), 1.239 (t, 3H), .
1.2 (d, 6H), 1.1 (t, 3H).
543 b 7.3 (d, 2H), 7.1 (d, 2H), 4.6-4.7 (m, 1H), 3.658 (s,
3H), 3.5 (t, 2H), 2.3-2.4 (t, 2H), 1.9-2.0 (m,
2H), 1.3 (d, 6H).
544 8 7.3 (d, 2H), 7.1 (d, 2H), 5.5 (t, 1H), 4.6-4.7 (m, 1H),
4.2 (d, 2H), 2.1 (s, 3H), 1.1 (d, 6H) (3:1
cis/trans mixture).
545 8 7.3 (d, 2H), 7.1 (d, 2H), 5.2 (t, 1H), 4.6-4.7 (m, 1H),
4.0 (d, 2H), 1.735 (s, 3H), 1.719 (s, 3H), 1.1
(d, 6H).
546 8 7.3 (d, 2H), 7.1 (d, 2H), 5.6-5.8 (m, 1H), 4.9 (m, 2H),
4.6-4.7 (m, 1H), 3.4 (t, 2H), 2.0-2.1 (q, 2H),
1.7-1.8 (m, 2H), 1.2 (d, 6H).
547 8 7.4-7.37 (m, 2H), 7.19-7.16 (m, 2H), 4.65 (m, 1H), 4.48
(q, 1H), 2.19 (s, 3H), 1.66 (d, 3H), 1.2 (d,
6H).
548 8 7.38-7.35 (m, 2H), 7.21-7.18 (m, 2H), 4.65 (m, 1H),
2.93 (s, 2H), 1.2 (d, 6H), 0.08 (s, 9H).
549 8 7.4 (d, 2H), 7.2 (d, 2H), 5.1 (s, 1H), 4.9 (s, 2H),
4.6-4.7 (m, 1H), 4.1-4.2 (q, 2H), 3.7-3.8 (q, 2H),
1.3 (t, 3H), 1.1-1.2 (m, 9H).
550 8 7.3 (d, 2H), 7.1 (d, 2H), 4.6-4.7 (m, 1H), 3.4-3.5 (d,
2H), 2.6-2.7 (m, 1H), 2.0-2.1 (m, 2H), 1.8-1.9
(q, 2H), 1.1 (d, 6H).
551 8 7.3 (d, 2H), 7.1 (d, 2H), 4.6-4.7 (m, 1H), 4.5 (t, 1H),
4.3-4.4 (t, 1H), 3.5 (t, 2H), 1.6-1.8 (m, 4H),
1.2 (d, 6H).
552 8 7.3 (d, 2H), 7.1 (d, 2H), 5.7-5.9 (m, 1H), 5.3-5.5 (m,
1H), 4.6-4.7 (m, 1H), 4.0 (d, 2H), 2.0-2.1 (m,
2H), 1.1 (d, 6H), 0.9 (t, 3H).
553 8 7.4 (d, 2H), 7.2 (d, 2H), 4.6-4.7 (m, 1H), 4.244 (s,
2H), 2.4 (q, 2H), 1.2 (d, 6H), 1.087 (t, 3H).
554 8 7.4 (d, 2H), 7.2 (d, 2H), 4.6-4.7 (m, 1H), 3.7 (t, 2H),
2.4-2.6 (m, 2H), 1.2 (d, 6H).
555 8 7.4 (d, 2H), 7.2 (d, 2H), 4.6-4.7 (m, 1H), 3.5 (t, 2H),
2.0-2.2 (m, 2H), 1.8-2.0 (m, 2H), 1.1 (d, 6H).
556 8 7.39 (m, 3H), 7.3 (m, 2H), 4.6-4.7 (m, 1H), 3.45 (t,
2H), 1.56 (m, 2H), 1.3 (m, 2H), 1.2 (d, 6H),
0.9 (t, 3H).
557 8 7.38 (m, 3H), 7.26 (m, 2H), 4.6-4.7 (m, 1H), 3.44 (t,
2H), 1.6 (m, 2H), 1.3 (m, 4H), 1.2 (d, 6H),
0.86 (t, 3H).
558 8 7.387 (m, 3H), 7.38 (m, 2H), 4.6-4.7 (m, 1H), 3.44 (t,
2H), 1.6 (m, 2H), 1.25 (d, 6H), 1.2 (s, 6H),
0.859 (t, 3H).
559 8 7.4 (m, 3H), 7.26 (m, 2H), 4.6-4.7 (m, 1H), 4.53 (t,
1H), 4.37 (t, 1H), 3.61-3.66 (t, 2H), 1.9-2.1
(m, 2H), 1.2 (d, 6H).
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560 8 7.37 (m, 3H), 7.26 (m, 2H), 4.87 (t, 1H), 4.6-4.7 (m,
1H), 3.8-3.9 (m, 2H), 3.7-3.8 (m, 2H)m 3.63
(t, 2H), 2.045 (m, 2H), 1.2 (d, 6H).
561 8 7.3 (m, 3H), 7.26 (m, 2H), 4.6-4.7 (m, 1H), 4.56 (t,
1H), 3.9-4.0 (m, 2H), 3.6 (m, 4H), 1.9 (m,
3H), 1.259 (t, 1H), 1.2 (d, 6H).
562 8 7.39 (m, 3H), 7.26 (m, 2H), 4.87 (s, 2H), 4.6-4.7 (m,
1H), 3.377 (s, 3H), 1.2 (d, 6H).
563 8 7.3 (m, 3H), 7.27 (m, 2H), 4.886 (s, 2H), 4.6-4.7 (m,
1H), 3.547-3.571 (q, 2H), 1.2 (d, 6H), 1.129-
1.15 (t, 3H).
564 8 7.38 (m, 3H), 7.26 (m, 2H), 4.966 (s, 2H), 4.6-4.7 (m,
1H), 3.7 (t, 2H), 3.4 (t, 2H), 3.257 (s, 3H),
1.2 (d, 6H).
565 8 7.39 (m, 3H), 7.26 (m, 2H), 4.6-4.7 (m, 1H), 4.046 (t,
2H), 3.495 (t, 2H), 2.033 (s, 3H), 1.6-1.8
(m, 4H), 1.2 (d, 2H).
566 8 7.38 (m, 3H), 7.26 (m, 2H), 4.6-4.7 (m, 1H), 3.66-3.707
(t, 2H), 2.6-2.7 (m, 2H), 1.2 (d, 6H).
567 8 7.38 (m, 3H), 7.24 (m, SH), 7.12 (d, 2H), 4.63 (m, 1H),
3.67 (t, 2H), 2.9 (t, 2H), 1.2 (d, 6H).
568 8 7.39 (m, 3H), 7.26 (m, 2H), 4.6-4.7 (m, 1H), 3.3 (d,
2H), 1.2 (d, 6H), 1.1 (m, 1H), 0.5 (q, 2H), 0.3
(q, 2H).
569 b 7.38 (m, 3H), 7.26 (m, 2H), 4.6-4.7 (m, 1H), 4.353 (s,
2H), 2.422 (s, 3H), 2.225 (s, 3H), 1.2 (d,
6H).
570 8 7.759 (d, 2H), 7.438 (t, 1H), 7.374 (t, 3H), 7.37 (m,
2H), 7.26 (m, 2H), 5.3-5.4 (q, 1H), 4.6-4.7 (m,
1H), 1.7 (d, 3H), 1.2 (d, 6H).
571 8 7.37 (m, 3H), 7.25 (m, 2H), 4.6-4.7 (m, iH), 4.2 (s,
2H), 3.2-3.3 (q, 2H), 3.3-3.4 (q, 2H), 1.2 (m,
9H), 1.1 (t, 3H).
572 8 7.39 (m, 3H), 7.26 (m, 2H), 4.6-4.7 (m, 1H), 3.6 (s,
3H), 3.54 (t, 2H), 2.3 (t, 2H), 1.9 (m, 2H), 1.2
(d, 6H).
573 8 7.39 (m, 3H), 7.26 (m, 2H), 5.5 (t, 1H), 4.6-4.7 (m,
1H), 4.2 (d, 2H), 2.1 (s, 3H), 1.2 (d, 6H).
574 8 7.39 (m, 3H), 7.26 (m, 2H), 5.1-5.2 (t, 1H), 4.6-4.7
(m, 1H), 4.01-4.039 (d, 2H), 1.7 (d, 6H), 1.2
(d, 6H).
575 8 7.39 (m, 3H), 7.26 (m, 2H), 5.6-5.8 (m, 1H), 4.9-5.1
(m, 2H), 4.6-4.7 (m, 1H), 3.44-3.49 (t, 2H),
2.0-2.1 (q, 2H), 1.7-1.8 (m, 2H), 1.2 (d, 6H).
576 8 7.39 (m, 3H), 7.26 (m, 2H), 4.6-4.7 (m, 1H), 4.4-4.5
(q, 1H), 2.166 (s, 3H), 1.6 (d, 2H), 1.2 (d,
6H).
577 8 7.37 (m, 3H), 7.26 (m, 2H), 4.6-4.7 (m, 1H), 2.9 (s,
2H), 1.2 (d, 6H), 0.6-0.8 (m, 9H).
578 8 7.4 (m, 3H), 7.26 (m, 2H), 5.1 (s, 1H), 4.862-4.866
(s, 2H), 4.6-4.7 (m, 1H), 4.1-4.2 (q, 2H), 3.7-
3.8 (q, 2H), 1.17-1.28 (m, 12H).
579 8 7.4-7.2 (m, lOH), 4.97 (s, 2H), 4.63 (m, 1H), 4.58 (s,
2H), 1.2 (d, 6H).
580 8 7.38 (m, 3H), 7.26 (m, 2H), 4.6-4.7 (m, 1H), 3.47-3.49
(d, 2H), 2.6-2.7 (m, 1H), 1.9-2.1 (m, 2H),
1.8-1.9 (q, 2H), 1.7-1.8 (q, 2H), 1.2 (d, 6H).
581 8 7.39 (m, 3H), 7.26 (m, 2H), 4.6-4.7 (m, 1H), 4.5 (t,
1H), 4.3-4.4 (t, 1H), 3.5 (t, 2H), 1.7-1.8 (m,
3H), 1.6-1.7 (m, 1H), 1.2 (d, 6H).
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582 8 7.38 (m, 3H), 7.26 (m, 2H), 5.7-5.9 (m, 1H), 5.3-5.4
(m, 1H), 4.6-4.7 (m, 1H), 4.0 (d, 2H), 1.9-2.1
(m, 2H), 1.2 (d, 6H), 0.9-1.0 (t, 3H).
583 b 7.39 (m, 3H), 7.26 (m, 2H),'4.6-4.7 (m, 1H), 4.23 (s,
2H), 2.45-2.48 (q, 2H), 1.2 (d, 6H), 1.1 (t,
3H).
584 8 7.39 (m, 3H), 7.26 (m, 2H), 4.6-4.7 (m, 1H), 3.7 (t,
2H), 2.4-2.6 (m, 2H), 1.2 (d, 6H).
585 8 7.3 (m, 2H), 7.1 (m, 2H), 4.6-4.7 (m, 1H), 3.5 (t, 2H),
2.0-2.2 (m, 2H), 1.8-2.0 (m, 2H), 1.2 (d,
6H).
587 8 7.4 (m, 3H), 7.3 (m, 2H), 4.6 (m, 1H), 4.1 (m, 4H),
3.8 (d, 2H), 1.2 (m, 12H).
592 8 7.4 (m, 2H), 7.2 (m, 2H), 5.1 (m, 1H), 4.7 (m, 1H),
3.3 (s, 3H), 1.7 (d, 3H), 1.2 (d, 6H).
593 S 7.3 (m, 1H), 6.9 (m, 2H), 5.1 (m, 1H), 4.7 (m, 1H),
3.3 (s, 3H), 1.7 (d, 3H), 1.2 (m, 6H).
594 8 7.28 (m, 1H), 6.92 (m, 2H), 4.6 (m, 1H), 4.2 (m, 1H),
3.8 (m, 1H), 3.4 (m, 1H), 1.31 (d, 3H), 1.26
(d, 6H).
596 8 7.22 (m, 2H), 7.09 (m, 2H), 4.65 (m, lh), 4.4 (m, 2H),
4.2-3.6 (m, 3H), 2.04 (s, 3H), 1.21 (d, 6H).
597 8 7.39 (m, 2H), 7.16 (m, 2H), 4.6 (m, 1H), 4.2-3.6 (m,
2H), 1.22 (d, 6H).
598 8 7.28 (m, 1H), 6.9 (m, 2H), 4.63 (m, 1H), 3.8 (s, 2H),
1.26 (b, 6H).
599 8 7.4 (d, 2H), 7.20 (d, 2H), 4.65 (m, 1H), 4.12 (q, 4H),
4.80 (d, 2H), 1.30 (m, 12H).
600 8 7.11 (m, 3H), 5.80 (m, 1H), 5.22 (m, 3H), 4.03 (d, 2H),
3.90 (m, 2H), 3.26 (s, 3H), 2.35 (d, 6H),
1.41 (d, 3H).
603 8 7.38-7.41 (m, 3H), 7.21-7.25 (m, 2H), 4.82-4.89 (m,
1H), 4.59-4.68 (m, 1H), 4.08-4.16 (m, 1H),
3.68-3.74 (m, 1H), 1.57 (d, 3H), 1.21 (d, 6H).
604 b 7.29-7.37 (m, 1H), 6.90-6.96 (m, 2H), 4.83-4.90 (m,
1H), 4.58-4.67 (m, 1H), 4.09-4.17 (m, 1H),
3.68-3.74 (m, 1H), 1.58 (d, 3H), 1.22 (br s, 6H).
605 8 7.6 (m, 1H), 7.48 (m, 1H), 7.3 (m, 3H), 7.2 (m, 3H),
5.94 (s, 1H), 5.3 (s, 1H), 4.6 (m, 3H), 1.2 (d,
6H).
606 8 7.4-7.2 (m, 7H), 6.9 (m, 2H), 5.4 (s, 1H), 5.1 (s, 1H),
4.7-4.6 (m, 1H), 4.4 (s, 2H), 1.2 (d, 6H).
607 b 7.4 (m, 3H), 7.3-7.2 (m, 2H), 4.9 (s, 1H), 4.8 (s, 1H),
4.7-4.6 (m, 1H), 3.9 (s, 2H), 1.7 (s, 3H), 1.2
(d, 6H).
608 8 7.4 (m, 3H), 7.2 (m, 2H), 5.4 (s, 2H), 4.7-4.6 (m, 1H),
4.2 (s, 2H), 1.2 (d, 6H).
609 8 7.39 (m, 3H), 7.26 (m, 2H), 4.82 (m, 1H), 4.64 (m, 1H),
2.41 (s, 1H), 1.60 (d, 3H), 1.22 (d, 6H).
614 8 7.4 (m, 3H), 7.2 (m, 2H), 4.6-4.7 (m, 1H), 4.0-4.2 (4H),
5.0 (m, 1H), 3.9 (m, 1H), 3.0-3.2 (q of q,
2H), 1.2 (m, 16H).
615 8 7.2 (m, 2H), 7.0-7.1 (t, 2H), 5.7 (m, 1H), 4.6 (m, 1H),
4.2 (m, 2H), 3.9 (m, 2H), 3.0-3.2 ( m, 2I~,
1.1-1.3 (m, 14H).
616 8 7.2-7.3 (m, 2H), 7.0-7.1 (m, 2H), 4.6-4.7 (m, 2H), 3.7
(s, 3H), 1.66 (d, 3H), 1.2 (d, 6H).
617 8 7.3 (m, 2H), 7.1 (m, 2H), 4.6 (m, 1H), 4.3 (m, 1H),
4.1 (m, 4H), 1.6 (m, 6H), 1.2 (m, 12H).
623 8 7.4 (d, 2H), 7.2 (d, 2H), 4.6-4.7 (m, 2H), 3.742 (s,
3H), 1.6 (d, 3H), 1.2 (d, 6H).
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627 b 7.20 (m, 2H), 7.10 (m, 2H), 4.70 (m, 2H), 3.70 (m, 2H),
3.60 (t, 2H), 3.55 (t, 2H), 3.30 (s, 3H)
1.20 (d, 6H).
629 S 7.20 (m, 2H), 7.10 (m, 2H), 4.70 (m, 2H), 3.70 (m, 2H),
3.60 (d, 2H), 3.45 (m, 2H), 1.20 (d, 6H),
1.10 (t, 6H).
631 8 7.35 (m, 3H), 7.28 (m, 2H), 4.70 (m, 1H), 3.65 (t, 2H),
3.54 (t, 2H), 3.30 (s, 3H), 1.22 (d, 6H).
632 8 7.35 (m, 3H), 7.28 (m, 2H), 4.70 (m, 2H), 3.65 (m, 2H),
3.55 (d, 2H), 3.48 (m, 2H), 1.20 (d, 6H),
1.10 (d, 6H).
634 8 7.3 (m, 1H), 6.92 (m, 2H), 5.43 (s, 2H), 4.65 (m, 1H),
4.23 (s, 2H), 1.21 (bs, 6H).
635 b 7.3 (m, 1H), 6.9 (m, 2H), 4.62 (m, 1H), 3.46 (t, 2H),
1.56 (m, 2H), 1.2 (m, 8H), 0.91 (t, 3H).
636 S 7.3 (m, 1H), 6.9 (m, 2H), 4.64 (m, 1H), 3.45 (t, 2H),
1.64 (m, 2H), 1.2 (m, lOH), 0.87 (t, 3H).
637 8 7.3 (m, 1H), 6.9 (m, 2H), 4.63 (m, 1H), 3.45 (t, 2H),
1.6 (m, 2H), 1.2 (m, 12H), 0.86 (t, 3H).
639 8 7.37 (d, 2H), 7.17 (d, 2H), 4.64 (m, 1H), 4.43 (s, 2H),
1.91 (m, 1H), 1.2 (m, 8H), 1.04 (m, 2H).
640 8 7.21 (m, 2H), 7.09 (m, 2H), 4.65 (m, 1H), 4.19 (s, 2H),
3.3 (m, 1H), 2.4-1.8 (m, 6H), 1.21 (d, 6H).
642 8 7.34 (m, 1H), 6.94 (m, 2H), 4.65 (m, 1H), 4.19 (s, 2H),
3.3 (m, 1H), 2.4-1.8 (m, 6H), 1.21 (d, 6H).
643 8 7.37 (d, 2H), 7.17 (d, 2H), 4.65 (m, 1H), 4.19 (s, 2H),
3.3 (m, 1H), 2.4-1.8 (m, 6H), 1.21 (d, 6H).
648 8 7.3 (m, 2H), 7.2 (m, 3H), 5.0 (s, 1H), 4.8-4.6 (m, 1H),
4.5 (s, 1H), 4.0 (s, 2H), 1.2 (d, 6H).
649 8 7.3 (m, 3H), 7.2 (m, 2H), 4.9 (s, 1H), 4.8 (s, 1H),
4.7-4.6 (m, 1H), 4.0 (s, 2H), 2.3-2.1 (m, 1H), 1.2
(d, 6H), 1.0 (d, 6H).
650 8 7.4-7.0 (m, lOH), 5.0 (ABm, 2H), 4.7-4.6 (m, 1H), 3.9
(s, 2H), 3.3 (s, 2H), 1.2 (d, 6H).
651 8 7.3 (m, 3H), 7.2 (m, 2H), 6.5 (s, 1H), 5.9 (s, 1H),
5.0 (m, 1H), 4.7-4.6 (m, 1H), 3.66 (s, 3H), 1.5
(d, 3H), 1.2 (d, 6H).
652 b 7.3 (m, 3H), 7.2 (m, 2H), 5.6 (m, 1H), 5.4 (m, 1H),
4.7-4.6 (m, 1H), 2.4 (s, 1H), 1.73 (s, 3H), 1.69
(s, 3H), 1.2 (d, 6H).
655 b 7.4 (m, 3H), 7.2 (m, 2H), 6.4-6.3 (m, 1H), 5.6-5.5 (m,
1H), 4.7-4.6 (m, 1H), 2.9 (s, 1H), 1.6 (s,
6H), 1.2 (d, 6H).
656 b 7.22 (m, 2H), 7.09 (m, 2H), 4.63 (m, 2H), 3.95 (m, 2H),
2.07 (m, 2H), 1.94 (m, 2H), 1.60 (d, 3H),
1.18 (d, 6H).
657 8 7.40 (m, 1H), 6.94 (m, 2H), 4.82 (m, 1H), 4.64 (m, 1H),
2.40 (m, 1H), 1.60 (d, 3H), 1.20 (d, 6H).
658 b 7.39 (m, 2H), 7.20 (m, 2H), 4.80 (m, 1H), 4.64 (m, 1H),
2.42 (m, 1H), 1.64 (d, 3H), 1.21 (d, 6H).
672 S 7.26 (m, 2H), 7.09 (m, 2H), 4.67 (m, 1H), 4.4 (m, 1H),
3.9 (m, 2H), 3.8 (m, 2H), 1.22 (d, 6H).
675 8 7.35 (m, 1H), 6.93 (t, 2H), 4.6 (m, 1H), 3.62 (t, 2H),
2.39 (t, 2H), 2.05 (m, 2H), (br, 6H)
677 8 7.39 (m, SH) 7.20 (m, 2H), 7.10 (m, 2H), 5.60 (s, 1H),
4.60 (m, 1.20 (d, 6H), 3.78 (s, 3H), 1.19 (d,
6H).
681 8 7.3 (d, 2H), 7.2 (d, 2H), 5.0 (m, 1H), 4.6-4.7 (m, 1H),
4.0-4.2 (m, 4H), 3.0-3.3(m, 2H), 1.2-1.3(m,
12H).
682 8 7.56 (s, 1H), 7.36 (m, 1H), 6.91 (m, 2H), 4.60 (m, 1H),
4.47 (s, 2H), 4.15 (q, 2H), 1.41 (t, 3H),
1.21 (brs, 6H).
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683 8 7.54 (s, 1H), 7.38 (m, 3H), 7.24 (m, 2H), 4.63 (m, 1H),
4.59 (s, 2H), 4.14 (q, 2H), 1.41 (t, 3H),
1.21 (d, 6H).
684 8 7.56 (s, 1H), 7.36 (m, 2H), 7.19 (m, 2H), 4.63 (m, 1H),
4.48 (s, 2H), 4.15 (q, 2H), 1.41 (t, 3H),
1.19 (d, 6H).
685 8 7.56 (s, 1H), 7.22 (m, 2H), 7.07 (m, 2H), 4.63 (m, 1H),
4.48 (s, 2H), 4.15 (q, 2H), 1.41 (t, 3H),
1.19 (d, 6H).
686 8 7.68 (s, 1H), 7.22 (m, 2H), 7.07 (m, 2H), 5.12 (q, 1H),
4.63 (m, 1H), 4.14 (q, 2H), 1.73 (d, 3H),
1.41 (t, 3H), 1.18 (d, 6H).
687 8 7.37 (m, IH), 6.92 (m, 2H), 4.62 (m, 1H), 3.81 (t, 2H),
2.94 (s, 3H), 2.92 (s, 3H), 2.66 (t, 2H),
1.22 (m, 6H).
693 b 9.52 (s, IH), 7.22 (m, 3H), 7.1 (m, 2H), 4.64 (m, 1H),
4.44 (q, 1H), 1.6 (d, 3H), 1.2 (d, 6H).
694 8 7.37 (m, 1H), 6.92 (m, 2H), 5.99 (m, 1H), 5.44 (m, 1H),
4.64 (m, 1H), 4.57 (m, 1H), 2.2-1.6 (m,
6H), 1.21 (br, 6H).
696 8 7.37 (d, 2H), 7.17 (d, 2H), 5.99 (m, 1H), 5.44 (m, 1H),
4.64 (m, 1H), 4.57 (m, 1H), 2.2-1.6 (m,
6H), 1.21 (d, 6H).
697 8 7.4 (m, 3H), 7.15 (m, 2H), 4.65 (m, 1H), 3.90 (m, 8H),
2.20 (m, 2H), 1.22 (d, 6H).
698 8 7.4 (d, 2H), 7.20 (d, 2H), 4.65 (m, 1H), 3.90 (m, 8H),
2.20 (m, 2H), 1.22 (d, 6H).
701 8 7.35 (d, 2H), 7.20 (d, 2H), 4.65 (m, IH), 3.90 (m, 1H),
2.85 (m, 1H), 1.40-2.00 (m, 6H), 1.20 (d,
9H).
702 8 7.40 (m, 1H), 6.92 (m, 2H), 4.65 (m, 1H), 3.90 (m, 1H),
2.85 (m, 1H), 1.40-2.00 (m, 6H), 1.25 (m,
9H).
705 8 7.22 (m, 2H), 7.06 (m, 2H), 4.78 (q, 1H), 4.62 (m, 1H),
3.64 (m, 8H), 1.66 (d, 3H), 1.19 (d, 6H).
708 8 7.29 (m, 1H), 6.92 (m, 2H), 4.65 (m, 1H), 4.4-3.5 (m,
SH), 2.04 (s, 3H), 1.23 (bs, 6H).
712 8 7.28 (m, 2H), 7.08 (m, 2H), 4.62 (m, 1H), 3.52 (m, 4H),
1.8 (m, 4H), 1.18 (d, 6H).
713 8 7.23 (m, 2H), 7.08 (m, 2H), 4.61 (m, 1H), 3.66 (t, 2H),
3.5 (t, 2H), 2.11 (m, 2H), 1.21 (d, 6H).
714 8 7.3 (m, 1H), 6.92 (m, 2H), 4.65 (m, 1H), 4.25 (m, 1H),
3.71 (m, 2H), 1.49 (d, 3H), 1.23 (bs, 6H).
715 8 7.40 (m, 1H), 6.92 (m, 2H), 4.65 (m, 1H), 3.90 (m, 1H),
3.56 (q, 2H), 3.30 (m, 2H), 1.82 (m, 1H),
1.50 (m, SH), 1.20 (m, 6H).
717 8 7.40 (m, 3H), 7.25 (m, 2H), 4.65 (m, 1H), 3.90 (m, 1H),
2.85 (m, 1H), 1.50-2.00 (m, 6H), 1.25 (d,
3H), 1.20 (d, 6H)
718 8 7.25 (m, 2H), 7.10 (m, 2H), 4.65 (m, 1H), 3.90 (m, 1H),
2.85 (m, 1H), 1.50-2.00 (m, 6H), 1.25 (d,
3H), 1.20 (d, 6H).
720 8 7.3 (m, IH), 6.9 (m, 2H), 4.6 (m, IH), 3.1 (m, 1H),
1.5 (m, 3H), 1.4 (m, 1H), 1.2 (m, 6H), 0.6-0.3
(m, 4H).
721 8 7.22 (m, 2H), 7.09 (m, 2H), 4.92 (m, 1H), 4.65 (m, 1H),
4.39 (m, 2H), 2.91 (m, 2H), 1.68 (d, 3H),
1.19 (d, 6H).
723 b 7.39 (m, 7H) 7.20 (m, 2H), 7.10 (m, 2H), 5.60 (s, 1H),
4.60 (m, 1H), 3.78 (s, 3H), 1.19 (d, 6H).
724 8 7.40 (m, 7H), 7.15 (d, 2H), 5.60 (s, IH), 4.60 (m, IH),
3.79 (s, 3H), 1.20 (d, 6H).
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725 8 7.4 (m, 2H), 7.2 (m, 2H), 5.1 (m, 1H), 4, 6 (m, iH),
4.1 (m, 1H), 3.8 (m, 1H), 3.4 (s, 3H), 1.2 (d,
6H).
726 8 7.4 (m, 2H), 7.2 (m, 2H), 5.1 (m, 1H), 4, 6 (m, 1H),
4.1 (m, 1H), 3.9 (m, 1H), 3.4 (s, 3H), 3.3 (s,
3H), 1.2 (d, 6H).
727 8 7.2 (m, 2H), 7.1 (m, 2H), 5.97 br, 1H), 4.65 (m, 1H),
3.65 (m, 2H), 3.45 (m, 2H), 1.91 (s, 3H),
1.19 (d, 6H).
729 8 7.39 (m, 3H), 7.25 (m, 2H), 4.91 (q, 1H), 4.64 (m, 1H),
4.37 (m, 2H), 2.92 (m, 2H), 1.67 (d, 3H),
1.20 (d, 6H).
730 8 7.35 (m, 1H), 6.93 (m, 2H), 4.93 (q, 1H), 4.65 (m, 1H),
4.39 (m, 2H), 2.94 (m, 2H), 1.68 (d, 3H),
1.20 (d, 6H).
731 b 8.4 (s, 1H), 7.6 (m, 1H), 7.5 (m, 1H), 7.4 (m, 3H),
7.2 (m, 2H), 5.84 (s, 1H), 5.3 (s, 1H), 4.7 (m,
1 H), 4.6 (s, 2H), 1.2 (d, 6H).
732 8 7.3-7.2 (m, 3H), 7.1-7.0 (m, 2H), 6.4 (s, 1H), 5.7 (s,
1H), 4.7-4.6 (m, 1H), 4.3 (s, 2H), 3.75 (s,
3H), 1.2 (d, 6H).
734 8 7.4 (m, 3H), 7.2 (m, 2H), 5.1 (m, 1H), 4, 6 (m, 1H),
4.1 (m, 1H), 3.9 (m, 1H), 3.4 (s, 3H), 3.3 (s,
3H), 1.2 (d, 6H).
735 S 7.4 (m, 3H), 7.2 (m, 2H), 5.1 (m, 1H), 4, 6 (m, 1H),
4.1 (m, 1H), 3.8 (m, 1H), 3.4 (s, 3H), 1.2 (d,
6H).
737 8 7.3 (m, 1H), 6.9 (m, 2H), 5.1 (m, 1H), 4, 6 (m, 1H),
4.1 (m, 1H), 3.8 (m, 1H), 3.4 (s, 3H), 1.2 (d,
6H).
738 8 7.3 (m, 1H), 6.9 (m, 2H), 5.1 (m, 1H), 4, 6 (m, 1H),
4.1 (m, 1H), 3.9 (m, 1H), 3.4 (s, 3H), 3.3 (s,
3H), 1.2 (d, 6H).
742 8 7.3 (m, 1H), 6.9 (m, 2H), 4.9 (m, 1H), 4.7 (m, 1H),
3.4-3.6 (m, 2H), 2.1 (m, 1H), 1.9 (m, lh), 1.2
(m, 9H), 0.9 (t, 3H).
744 8 7.40 (m, 1H), 6.92 (m, 2H), 4.66 (m, 1H), 3.67 (m, 2H),
2.56 (m, 2H), 1.95 (m, 1H), 1.60 (d, 6H).
746 8 7.41 (m, 3H), 7.39 (m, 2H), 5.60 (m, 1H), 4.62 (m, 1H),
3.82 (m, 2H) 1.20 (d, 6H).
747 8 7.38 (m, 3H) 7.25 (m, 2H), 4.66 (m, 1H), 4.25 (m, 1H),
3.65 (m, 2H), 1. 49 (d, 3H), 1.20 (d, 6H).
748 8 7.39 (m, 2H) 7.17 (m, 2H), 4.62 (m, 1H), 4.25 (m, 1H),
3.65 (m, 2H), 1. 49 (d, 3H), 1.20 (d, 6H).
750 8 7.39 (m, 3H) 7.26 (m, 2H), 4.63 (m, 1H), 3.65 (m, 2H),
3, 48 (m, 2H), 2.10 (m, 2H), 1.20 (d, 6H).
753 8 7.22 (m, 2H), 7.11 (m, 2H), 4.64 (m, 1H), 4.58 (m, 1H),
2.42 (m, 1H), 2.04 (m, 1H), 1.94 (m, 1H),
1.20 (d, 6H), 0.99 (t, 3H).
758 S 1.20 (m, 6H), 4.07 (m, 2H), 4.17 (s, 2H), 4.32 (m, 2H),
4.62 (m, 1H), 6.92 (m, 2H), 7.36 (m, 1H).
759 8 7.38 (d, 2H), 7.18 (d, 2H), 4.92 (q, 1H), 4.62 (m, 1H),
4.39 (m, 2H), 2.91 (m, 2H), 1.68 (d, 3H),
1.20 (d, 6H).
763 8 7.40 (m, 1H), 6.92 (m, 2H), 4.66 (m, 1H), 3.67 (m, 2H),
2.56 (m, 2H), 1.95 (m, 1H), 1.60 (d, 6H).
764 8 7.38 (m, 1H), 6.93 (m, 2H), 4.62 (m, 1H), 4.25 (s, 2H),
2.37 (m, 1H), 1.25 (d, 6H)
765 8 1.20 (m, 6H), 4.24 (S, 2H), 4.25 (M, 2H), 4.38 (M, 2H),
4.63 (M, 1H), 7.09 (M, 2H), 7.24 (M,
2H).
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766 8 7.25 (m, 2H), 7.15 (m, 1H) , 4.95 (brs, 1H), 4.65 (m,
1H), 4.16 (m, 2H), 3.39 (s, 3H), 2.19 (m,
1H), 1.92 (m, 3H), 1.19 (d, 6H).
767 8 7.26 (m, 2H), 7.11 (m, 2H), 4.64 (m, 1H), 3.67 (t, 2H),
2.56 (m,2H), 1.96 (m,lH), 1.21 (d, 6H).
768 8 7.38 (m, 3H), 7.26 (m, 2H), 4.64 (m, 1H), 3.66 (t, 2H),
2.54 (m, 2H), 1.92 (m,lH), 1.22 (d, 6H).
769 8 7.39 (m, 3H), 7.24 (m, 2H), 4.74 (s, 2H), 4.62 (m, 1H),
3.18 (m, 1H), 1.35 (d, 6H), 1.21 (d 6H).
771 8 8.3 (d, 1H), 7.6 (dd, 1H), 7.4 (d, 1H), 4.7 (septet,
1H), 4.2 (septet, 1H), 1.40 (d, 3H), 1.21 (d, 3H).
772 8 7.4 (m, 2H), 7.2 (m, 2H), 4.9 (m, 1H), 4.7 (m, 1H),
3.4-3.6 (m, 2H), 2.1 (m, 1H), 1.9 (m, 1H), 1.2
(m, 9H), 0.9 (t, 3H).
773 8 7.4 (m, 2H), 7.2 (m, 2H), 4.9 (m, 1H), 4.7 (m, 1H),
3.4-3.6 (m, 2H), 2.1 (m, 1H), 1.9 (m, 1H), 1.2
(m, 9H), 0.9 (t, 3H).
774 b 7.3 (m, 1H), 6.9 (m, 2H), 4.9 (m, 1H), 4.7 (m, 1H),
3.4-3.6 (m, 2H), 2.1 (m, 1H), 1.9 (m, 1H), 1.2
(m, 9H), 0.9 (t, 3H).
776 8 7.3 (m, 1H), 6.90 (m, 2H), 4.65 (m, 1H), 4.20 (m, SH),
1.70 (m, 3H), 1.25 (m, 12H).
778 8 7.4 (m, 1H), 6.90 (m, 2H), 4.65 (m, 1H), 3.60 (m, 7H),
2.85 (m, 3H), 1.21 (m, 6H).
779 8 7.4 (d, 2H), 7.2 (d, 2H), 4.65 (m, 1H), 3.60 (m, 7H),
2.85 (m, 3H), 1.21 (m, 6H).
782 8 7.22 (m, 2H), 7.09 (t, 2H), 5.93 (t, 1H), 4.62 (m, 1H),
4.21 (d, 2H), 1.2 (d, 6H).
783 8 7.38 (m, 1H), 6.96 (m, 2H), 4.60 (m, 2H), 2.40 (m, 1H),
2.10-1.80 (m, 2H), 1.22 (m, 1H), 0.94 (m,
3H).
784 8 7.39 (m, 2H), 7.20 (m, 2H), 4.64 (m, 1H), 4.25 (m, 2H),
2.33 (m, lI~, 1.21 (d, 6H).
785 8 7.35 (m, 1H), 6.92 (m, 2H), 5.32 (q, 1H), 4.62 (m, 1H),
2.31 (s, 3H), 2.24 (s, 3H), 1.83 (d, 3H),
1.22 (br, 6H).
792 b 7.39 (m, 3H) 7.25 (m, 2H), 4.61 (m, 1H), 3.52 (m, 4H),
1.80 (m, 4H), 1.20 (d, 6H).
797 8 7.4 (m, 3H), 7.3-7.1 (m, 2H), 5.5 (bs, 1H), 4.7-4.6
(m, 1H), 3.94 (bs, 2H), 2.35 (s, 2H), 2.3-2.2 (m,
2H), 2.0 (m, 2H), 1.2 (d, 6H), 1.2 (s, 6H).
800 8 7.38 (m, 3H), 7.25 (m, 2H), 4.64 (m, 1H), , 2.35 (m,
1H), 1.21 (d, 6H), 1.15 (s, 3H), 1.05 (m, 1H),
0.94 (m, 4H).
801 8 7.37 (d, 2H), 7.19 (d, 2H), 4.64 (m, 1H), 2.37 (m, 1H),
1.19 (m, 9H), 1.07 (m, 1H), 0.96 (m, 4H).
802 8 7.37 (m, 1H), 6.91 (m, 2H), 4.64 (m, 1H), 2.37 (m, 1H),
1.19 (m, 9H), 1.07 (m, 1H), 0.96 (m, 4H).
803 8 7.39 (m, 3H), 7.26 (m, 2H), 4.64 (m, 1H), 4.52 (m, 1H),
2.40 (m, 1H), 2.04 (m, 1H), 1.92 (m, 1H),
1.44 and 0.98 (t, 3H), 1.22 (d, 6H).
804 8 7.38 (m, 2H), 7.21 (m, 2H), 4.64 (m, 1H), 3.67 (t, 2H),
2.56 (m, 2H), 1.96 (m, 1H), 1.22 (d, 6H).
805 8 7.25 (m, 2H), 7.08 (m, 2H), 4.65 (m, 1H), 4.40 (m, 1H),
3.70 (m, 4H), 1.20 (d, 6H).
808 8 7.39 (m, 2H), 7.20 (m, 2H), 7.64 (m, 1H), 4.58 (m, 1H),
2.43 (m, 1H), 2.40 (m, 1H), 1.92 (m, 1H),
1.21 (d, 6H), 0.97 (t, 3H).
810 b 7.22 (m, 2H), 7.09 (m, 2H), 4.46 (m, 1H), 4.95 (m, 1),
4.64 (m, 1H), 3.02 (m, 1H), 2.76 (m, 1H),
1.68 (d, 3H), 1.20 (d, 6H).
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811 8 7.21 (m, 2H) , 7.11 (m, 2H), 4.98 (m, 1H), 4.64 (m,
1H), 3.89 (m, 1H), 2.98 (dd, 1H), 2.69 (dd,
1H), 1.5 (d, 3H), 1.20 (d, 6H).
812 8 7.42 (m, 3H), 7.40 (m, 2H), 5.44 (m, 1H), 4.93 (m, 1H),
4.64 (m, 1H), 2.80 (m, 1H), 2.70 (m, 1H),
1.28 (d, 3H), 1.22 (d, 6H).
814 8 7.39 (d, 2H), 7.17 (d, 2H), 7.11 (brs, 1H), 4.92 (m,
1H), 4.64 (m, 1H), 3.89.(m, 1H), 3.02 (m, 1H),
2.70 (m, 1H), 1.52 (d, 3H), 1.20 (d, 6H).
815 8 7.32 (m, 1H), 7.11 (brs, 1H), 6.94 (m, 2H), 4.88 (m,
1H), 4.64 (m, 1H), 3.90 (m, 1H), 3.01 (m,
1H), 2.70 (m, 1H), 1.51 (d, 3H), 1.23 (br, 6H).
816 8 7.40 (m, 3H), 7.23 (m, 2H), 7.09 (brs, 1H), 4.91 (m,
1H), 4.66 (m, 1H), 3.88 (m, 1H), 3.00 (m,
1H), 2.70 (m, 1H), 1.50 (d, 3H), 1.21 (d, 6H).
817 8 7.28 (m, 1H), 6.91 (m, 2H), 4.63 (m, 1H), 4.11 (m, iH),
1.28 (d, 3H), 1.22 (d, 6H).
819 8 7.22 (m, 2H), 7.08 (m, 2H), 4.62 (m, 1H), 3.78 (d, 1H),
3.50 (d, 1H), 2.70 (d, 1H), 2.60 (d, 1H),
1.33 (s, 3H), 1.18 (d, 6H).
822 8 7.40 (m, 2H), 6.92 (m, 2H), 4.60 (m, 1H), 3.66 (m, 2H),
3.50 (m, 2H), 2.05 (m, 2H), 1.26 (d, 6H).
823 8 7.40 (m, 2H), 6.92 (m, 2H), 4.61 (m, 1H), 3.54 (m, 4H),
1.80 (m, 4H), 1.22 (d, 6H).
824 b 7.39 (m, 3H), 7.24 (m, 2H), 4.62 (m, 1H), 4.30 (m, 1H),
3.90 (m, 1H), 3.70 (m, 1H), 3.60 (m, 1H),
3.30 (s, 3H), 1.22 (d, 6H).
825 S 7.21 (m, 2H), 7.08 (m, 2H), 4.62 (m, 1H), 4.30 (m, 1H),
3.90 (m, 1H), 3.71 (m, 1H), 3.60 (m, 1H),
3.30 (s, 3H), 1.22 (d, 6H).
829 8 4.66 (s, 1H), 4.5 (m, 1H), 4.3 (m, 1H), 1.48 (d, 6H),
1.42 (s, 9H), 1.28 (d, 6H).
837 8 7.20 (m, 2H), 7.10 (m, 2H), 5.65 (m, 2H), 5.05 (d, 1H),
4.65 (m, 1H), 4.20 (m, 4H), 1.45 (d, 3H),
1.20 (d, 6H).
839 8 7.12-7.2 (m, 3H), 4.62 (m, 1H), 4.17 (m, 1H), 1.39 (d,
6H), 1.25 (d, 6H).
840 8 7.23 (m, 2H), 7.1 (m, 2H), 4.2 (m, 1H), 3.80 (q, 2H),
1.40 (d, 6H), 1.27 (t, 3H).
841 8 7.38 (d, 2H), 7.18 (d, 2H), 6.0 (m, 1H), 5.25 (m, 2H),
4.6 (m, 2H), 1.5 (d, 3H), 1.2 (d, 6H).
842 8 7.38 (d, 2H), 6.93 (m, 2H), 5.98 (m, 1H), 5.24 (m, 2H),
4.6 (m, 2H), 1.49 (d, 3H), 1.22 (br, 6H).
843 8 7.4 (m, 3H), 7.25 (m, 2H), 6.0 (m, 1H), 5.22 (m, 2H),
4.6 (m, 2H), 1.48 (d, 3H), 1.2 (d, 6H).
845 8 7.38 (d, 2H), 6.93 (m, 2H), 4.9 (s, 2H), 4.64 (m, 1H),
4.41 (m, 1H), 3.45 (m, 2H), 2.95 (m, 2H),
1.21 (d, 6H).
846 8 7.4 (m, 3H), 7.25 (m, 2H), 4.89 (s, 2H), 4.64 (m, 1H),
4.41 (m, 1H), 3.45 (m, 2H), 2.95 (m, 2H),
1.21 (d, 6H).
849 8 9.53 (s, 1H), 7.39 (d, 2H), 7.19 (d, 2H), 4.64 (m, 1H),
4.44 (q, 1H), 1.6 (d, 3H), 1.21 (d, 6H).
850 8 9.51 (s, 1H), 7.4 (d, 3H), 7.25 (m, 2H), 4.64 (m, 1H),
4.42 (q, 1H), 1.58 (d, 3H), 1.21 (d, 6H).
852 8 7.42 (s,lH), 7.37 (m, 2H), 7.18 (m, 2H), 4.63 (m, 1H),
4.48 (s, 2H), 3.81 (s, 3H), 1.20 (d, 6H).
853 8 7.44 (s, 1H), 7.38 (m, 2H), 7.24 (m, 3H), 4.63 (m, 1H),
4.47 (s, 2H), 3.80 (s, 3H), 1.20 (d, 6H).
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854 8 7.47 (s, 1H), 7.37 (m, 1H), 6.93 (m, 2H), 4.62 (m, 1H),
4.49 (s, 2H), 3.81 (s, 3H), 1.21 (brs, 6H).
866 b 7.34 (m, 2H), 6.91 (m, 2H), 5.33 (m, 1H), 4.62 (m, 1H),
3.92 (s, 2H), 1.91 (m, 3H), 1.21 (brs, 6H).
871 8 7.40 (m, 2H), 7.19 (m, 2H), 4.65 (m, 1H), 4.30 (m, 1H),
3.95 (dd, 1H), 3.75 (m, 1H), 3.60 (m,
1H), 3.30 (s, 3H), 1.22 (d, 6H).
872 8 7.30 (m, 1H), 6.92 (m, 2H), 4.62 (m, 1H), 4.30 (m, 1H),
3.90 (m, 1H), 3.73 (m, 2H), 3.60 (m, 1H),
3.30 (s, 3H), 1.26 (d, 6H).
876 8 7.36 (m, 2H), 7.17 (m, 2H), 4.60 (m, 1H), 4.12 (m, 1H),
1.20 (d, 3H), 1.19 (d, 6H).
882 8 7.38 (m, 3H), 7.25 (m, 2H), 4.62 (m, 2H), 2.40 (m, 1H),
2.00-1.80 (m, 2H), 1.50-1.30 (m, 2H),
1.20 (d, 6H), 0.92 (t, 3H).
884 8 7.23 (m, 2H), 7.08 (m, 2H), 5.75 (m, 1H), 5.21 (m, 2H),
4.65 (m, 1H), 4.41 (s, 1H), 4.32 (s,lH),
4.25 (s, 1H), 3.98 ( s, 1H), 3.91 (d, 1H), 3.86 (s, 1.SH),
3.78 (d, 1H), 3.74 (s, 1.SH), 1.20 (d, 6H).
synlanti mixture
885 8 7.37 (m, 3H), 7.26 (m, 2H), 5.75 (m, 1H), 5.20 (m, 2H),
4.63 (m, 1H), 4.39 (s, 1H), 4.31 (s, 1H),
4.24 (s, 1H), 3.94 (s, 1H), 3.89 (d, 1H), 3.84 (s, 1.SH),
3.75 (d, 1H), 3.73 (s, 1.SH), 1.20 (d, 6H).
synlanti mixture
886 8 7.36 (m, 1H), 6.91 (m, 2H), 5.80 (m, 1H), 5.21 (m, 2H),
4.63 (m, 1H), 4.40 (s, 1H), 4.32 (s, 1H),
4.25 (s, 1H), 3.96 (s, 1H), 3.92 (d, 1H), 3.85 (s, 1.SH),
3.80 (d, 1H), 3.73 (s, 1.SH), 1.20 (br, 6H)
synlanti mixture
887 S 7.36 (d, 2H), 7.20 (d, 2H), 5.76 (m, 1H), 5.19 (m, 2H),
4.64 (m, 1H), 4.41 (s, 1H), 4.32 (s, 1H),
4.25 (s, 1H), 3.95 (s, 1H), 3.91 (d, 1H), 3.86 (s, 1.SH),
3.78 (d, 1H), 3.74 (s, 1.SH), 1.20 (d, 6H).
synlanti mixture
888 8 7.4 (d, 2H), 7.29 (d, 2H), 4.63 (m, 1H), 4.15 (m, 1H),
3.58 (m, 2H), 1.49-1.27 (m, 9H).
892 S 7.20 (m, 2H), 7.08 (t, 2H), 4.65 (m, 1H), 3.70 (m, 1H),
3.42 (m, 2H), 3.30 (m, 2H), 3.12 (s, 3H),
1.90 (m, 3H), 1.50 (m, 1H), 1.20 (m, 6H).
898 8 7.20 (m, 2H), 7.08 (t, 2H), 4.97 (d, 1H), 4.65 (m, 1H),
3.90 (m, 2H), 3.80 (m, 1H), 3.62 (m, 1H),
3.47 m, 1H , 1.50 m, 4H , 1.40 d, 3H , 1.20 m, 6H .
900 8 7.30 (m, 9H), 4.63 (m, 1H), 4.44 (s, 1H), 4.39 (s, 1H),
4.34 (s, 1H), 4.29 (s, 1H), 4.25 (s, 1H), 3.96
(s, 1H), 3.83 (s, 1.SH), 3.71 (s, 1.SH), 1.21 (m, 6H).
synlanti mixture
901 S 7.30 (m, lOH), 4.63 (m, 1H), 4.44 (s, 1H), 4.39 (s,
1H), 4.34 (s, 1H), 4.29 (s, 1H), 4.25 (s, 1H),
3.96 (s, 1H), 3.83 (s, 1.SH), 3.71 (s, 1.SH), 1.21(m,6H).
synlanti mixture
902 8 7.23 (m, 2H), 7.08 (m, 2H), 4.65 (m, 1H), 4.39 (s, 1H),
4.29 (s, 1H), 4.20 (s, 1H), 3.91 (s, 1H),
3.86 (s, 1.SH), 3.74 (s, 1.SH), 3.28 (s, 1.SH), 3.14 (s,
1.SH), 1.20 (d, 6H). synlanti mixture
903 8 7.37 (m, 3H), 7.26 (m, 2H), 4.64 (m, 1H), 4.38 (s, 1H),
4.28 (s, 1H), 4.19 (s, 1H), 3.89 (s, 1H),
3.85 (s, 1.SH), 3.74 (s, 1.SH), 3.27 (s, 1.SH), 3.10 (s,
1.SH), 1.20 (d, 6H). synlanti mixture
904 8 7.37 (m, 3H), 7.26 (m, 2H), 4.64 (m, 1H), 4.38 (s, 1H),
4.28 (s, 1H), 4.19 (s, 1H), 3.89 (s, 1H),
3.85 (s, 1.SH), 3.74 (s, 1.SH), 3.27 (s, 1.SH), 3.10 (s,
1.SH), 1.20 (d, 6H). 4:1 synlanti mixture
CA 02359108 2001-07-18
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905 8 7.35 (d, 2H), 7.27 (d, 2H), 4.39 (m, 2H), 4.15 (m, 1H),
3.40 (s, 3H), 3.38 (s, 3H), 1.39 (d, 6H),
1.26 (d, 3H).
908 8 7.36 (m, 3H), 7.26 (m, 2H), 4.35 (m, 2H), 4.15 (m, 1H),
1.70 (d, 3H), 1.38 (m, 6H).
909 8 7.28 (m, 2H), 7.09 (m, 2H), 4.38 (m, 2H), 4.18 (m, 1H),
1.68 (d, 3H), 1.38 (m, 6H).
913 8 7.4 (m, 3H), 7.25 (m, 2H), 4.64 (m, 1H), 3.71 (t, 2H),
2.84 (t, 2H), 2.14 (s, 3H), 1.21 (d, 6H).
914 8 9.73 (s, 1H), 7.22 (m, 2H), 7.09 (m, 2H), 4.64 (m, 1H),
3.81 (t, 2H), 2.88 (t, 2H), 1.2 (d, 6H).
915 8 7.35 (m, 1H), 6.92 (m, 2H), 4.63 (m, 1H), 3.51 (t, 2H),
2.45 (t, 2H), 2.11 (s, 3H), 1.89 (m, 2H),
1.22 (br, 6H).
916 8 7.37 (m, 2H), 7.18 (m, 2H), 4.64 (m, 1H), 3.51 (t, 2H),
2.45 (t, 2H), 2.11 (s, 3H), 1.89 (m, 2H),
1.22 (br, 6H).
917 8 7.37 (m, 2H), 7.21 (m, 2H), 4.62 (m, 2H), 2.40 (m, 1H),
2.00-1.80 (m, 2H), 1.50-1.30 (m, 2H),
1.20 (d, 6H), 0.92 (t, 3H).
919 8 7.34 (m, SH), 4.42 (m, 2H), 4.18 (m, 1H), 3.74 (s, 3H),
3.42 (s, 3H), 1.37 (d, 6H), 1.27 (m, 3H).
920 8 7.30 (m, 2H), 7.09 (m, 2H), 4.38 (m, 2H), 4.18 (m, 1H),
3.41 (s, 3H), 3.38 (s, 3H), 1.39 (d, 6H),
1.27 (m, 3H).
922 8 7.36 (d, 2H), 7.20 (d, 2H), 4.64 (m, 1H), 4.39 (s, 1H),
4.29 (s, 1H), 4.20 (s, 1H), 3.91 (s, 1H), 3.86
(s, 1.SH), 3.74 (s, 1.SH), 3.28 (s, 1.SH), 3.14 (s, 1.SH),
1.20 (d, 6H). synlanti mixture
923 8 7.38 (m, 1H), 6.91 (m, 2H), 4.64 (m, 1H), 4.39 (s, 1H),
4.29 (s, 1H), 4.19 (s, 1H), 3.91 (s, 1H),
3.86 (s, 1.SH), 3.74 (s, 1.SH), 3.29 (s, 1.SH), 3.15 (s,
1.SH), 1.20 (br, 6H). synlanti mixture
927 8 7.37 (m, 2H), 6.91 (m, 2H), 6.15 (m, 1H), 5.55 (m, 1H),
5.00 (m, 1H), 4.64 (m, 1H), 2.7 (m, 1H),
2.30 (m, 2H), 1.98 (m, 1H), 1.2 (br, 6H).
929 8 7.4 (m, 3H), 7.25 (m, 2H), 6.17 (m, 1H), 5.55 (m, 1H),
5.00 (m, 1H), 4.64 (m, 1H), 2.7 (m, 1H),
2.3 (m, 2H), 1.99 (m, 1H), 1.2 (d, 6H).
930 8 7.24 (m, 3H), 7.10 (m, 2H), 4.65 (m, 2H), 3.8 (m, 2H),
3.39 (m, 2H), 1.21 (d, 6H).
935 b 7.35 (m, 1H), 6.91 (m, 2H), 4.63 (m, 1H), 3.74 (t, 2H),
2.85 (t, 2H), 2.15 (s, 3H), 1.21 (br, 6H).
947 8 7.31 (m, 1H), 6.89 (m, 2H), 4.6 (m, 1H), 3.75 (m, 1H),
2.72 (m, 4H), 2.4 (m, 2H), 2.00 (m, 2H),
1.23 (m, 6H).
952 8 7. 51 (m, 3H), 7.24 (m, 2H), 6.86 (q, 1H), 4.31 (m,
1H), 1.97 (d, 3H), 1.49 (d, 6H).
953 8 7.34 (m, SH), 4.22 (m, 1H), 2.14 (s, 3H), 1.92 (s, 3H),
1.44 (d, 6H).
955 b 7.43 (m, SH), 4.64 (m, 1H), 4.17 (m, 1H), 3.79 (d, 4H),
1.38 (d, 6H).
956 8 7.44 (m, 2H), 7.12 (m, 2H), 4.19 (m, 1H), 4.13 (m, 2H),
3.78 (d, 4H), 1.40 (d, 6H).
959 b 7.38 (m, 3H), 7.26 (m, 2H), 4.64 (m, 1H), 4.26 (m, 1H),
2.41 (m, 2H), 1.22 (m, 6H), 1.10 (d, 3H),
0.85 (d, 3H).
962 8 7.22 (m, 2H), 7.10 (m, 2H), 4.64 (m, 1H), 3.51 (t, 2H),
2.45 (t, 2H), 2.11 (s, 3H), 1.90 (m, 2H), 1.2
(d, 6H).
CA 02359108 2001-07-18
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963 8 7.39 (m, 3H), 7.26 (m, 2H), 4.64 (m, 1H), 3.50 (t,
2H), 2.43 (t, 2H), 2.11 (s, 3H), 1.89 (m, 2H), 1.2
(d, 6H).
964 8 9.73 (s, 1H), 7.37 (m, 1H), 6.93 (m, 2H), 4.63 (m,
1H), 3.81 (t, 2H), 2.89 (t, 2H), 1.22 (br, 6H).
965 8 9.72 (s, 1H), 7.39 (m, 3H), 7.25 (m, 2H), 4.64 (m,
1H), 3.79 (t, 2H), 2.87 (t, 2H), 1.21 (br, 6H).
967 8 7.22 (m, 2H), 7.08 (m, 2H), 4.64 (m, 1H), 3.94 (m,
1H), 2.78 (m, 1H), 2.58 (m, 1H), 2.00-1.70 (m,
3H), 1.26 (m, 2H), 1.20 (m, 6H), 0.90 (m, 3H).
=1 ..1~~ ~~ ~~ ,~, ppm aownneia aom tetrametnyisitane. couplings are
designated by (s)-singlet,
(d)-doublet, (t)-triplet, (q)-quartet, (m)-multiplet, (dd)-doublet of
doublets, (dt)-doublet of triplets, (br s)-broad
singlet.
TEST A
Seeds of barnyardgrass (Echinochloa crus-galli), crabgrass (Digitaria spp.),
morningglory (Ipomoea spp.), and velvetleaf (Abutilon theophrasti) were
planted into a
sandy loam soil and treated preemergence by soil drench with test chemicals
formulated in a
non-phytotoxic solvent mixture which includes a surfactant. At the same time,
these crop
and weed species were also treated postemergence sprayed to runoff , with test
chemicals
formulated in the same manner.
Plants ranged in height from two to eighteen cm and were in the one to two
leaf stage
for the postemergence treatment. Treated plants and untreated controls were
maintained in a
greenhouse for approximately eleven days, after which all treated plants were
compared to
untreated controls and visually evaluated for injury. Plant response ratings,
summarized in
Table A, are based on a 0 to 10 scale where 0 is no effect and 10 is complete
control.
Table A COMPOUND
Rate 2000 g/ha 1 2 3 10 42 43 52 53 99 114 127 128 136 137 177 183
Pre-emergence
Barnyardgrass 9 9 9 10 0 0 9 8 9 10 9 0 9 10 9 9
Crabgrass 9 2 3 9 0 1 10 9 10 10 8 0 10 10 9 5
Morningglory 0 0 0 1 0 0 0 0 2 6 0 0 0 3 0 0
Velvetleaf 0 0 0 2 0 0 0 0 3 6 0 0 0 5 1 0
Table A COMPOUND
Rate 2000 g/ha 184 225 377 386
Pre-emergence
Barnyardgrass 9 10 0 0
Crabgrass 9 10 0 0
Morningglory 0 8 0 0
Velvetleaf 0 7 0 0
Table A COMPOUND
Rate 1000 g/ha 1 2 3 10 42 43 52 53 99 114 127 128 136 137 177 183
Barnyardgrass 8 8 6 9 0 0 5 3 7 8 6 0 4 8 0 0
Crabgrass 5 0 0 8 0 0 8 6 7 7 7 0 6 8 3 1
Morningglory 0 0 0 0 0 0 1 0 2 10 0 0 9 10 0 0
Velvetleaf 0 0 0 4 0 0 1 1 2 5 0 0 2 2 2 0
CA 02359108 2001-07-18
WO 00/43377 PCT/US00/01283
137
Table A COMPOUND
Rate 1000 g/ha184225 377386
Postemergence
Barnyardgrass 2 9 0 0
Crabgrass 1 9 0 0
Morningglory 10 10 0 0
Velvetleaf 2 3 0 0
TEST B
Seeds of bedstraw (Galium aparine), blackgrass (Alopecurus myosuroides),
Surinam
grass (Brachiaria decumbens), cocklebur (Xanthium strumarium), corn (Zea
mays),
crabgrass (Digitaria sanguinalis), giant foxtail (Setaria faberii),
morningglory (Ipomoea
hederacea), pigweed (Amaranthus retroy~lexus), rape (Brassica napus), soybean
(Glycine
max), sugar beet (Beta vulgaris), velvetleaf (Abutilon theophrasti), wheat
(Triticum
aestivum), wild oat (Avena fatua) and purple nutsedge (Cyperus rotundus)
tubers were
planted and treated preemergence with test chemicals formulated in a non-
phytotoxic solvent
mixture which included a surfactant.
At the same time, these crop and weed species were also treated with
postemergence
applications of test chemicals formulated in the same manner. Plants ranged in
height from
2 to 18 cm (1- to 4-leaf stage) for postemergence treatments. Plant species in
the flood test
consisted of rice (Oryza sativa), smallflower flatsedge (Cyperus difformis),
duck salad
1 S (Heteranthera limosa) and barnyardgrass (Echinochloa crus-galli) grown to
the 2-leaf stage
for testing. Treated plants and controls were maintained in a greenhouse for
twelve to
sixteen days, after which all species were compared to controls and visually
evaluated. Plant
response ratings, summarized in Table B, are based on a scale of 0 to 10 where
0 is no effect
and 10 is complete control. A dash (-) response means no test result.
CA 02359108 2001-07-18
WO 00/43377 PCT/US00/01283
138
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CA 02359108 2001-07-18
WO 00/43377 PCT/US00/01283
139
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CA 02359108 2001-07-18
WO 00/43377 PCT/US00/01283
140
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CA 02359108 2001-07-18
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307
TEST C
Compounds evaluated in this test were formulated in a non-phytotoxic solvent
mixture
which included a surfactant and applied to plants that were grown for various
periods of time
before treatment (postemergence application). A mixture of sandy loam soil and
greenhouse
potting mix in a 60:40 ratio was used for the postemergence test.
Plantings of these crops and weed species were adjusted to produce plants of
appropriate size for the postemergence test. All plant species were grown
using normal
greenhouse practices. Crop and weed species include arrowIeaf sida (Sida
rhombifolia),
barnyardgrass (Echinochloa crus-galli), cocklebur (Xanthium strumarium),
common
ragweed (Ambrosia elatior), corn (Zea mays), cotton (Gossypium hirsutum),
eastern black
nightshade (Solanum ptycanthum), fall panicum (Panicum dichotom~orum), field
bindweed
(Convolvulus arvensis), giant foxtail (Setaria faberii), hairy beggarticks
(Bidens pilosa),
ivyleaf morningglory (Ipomoea hederacea), johnsongrass (Sorghum halepense),
ladysthumb
smartweed (Polygonum persicaria), lambsquarters (Chenopodium album), large
crabgrass
(Digitaria sanguinalis), purple nutsedge (Cyperus rotundus), redroot pigweed
(Amaranthus
retroflexus), soybean (Glycine max), Surinam grass (Brachiaria decumbens),
velvetleaf
(Abutilon theophrasti) and wild poinsettia (Euphorbia heterophylla).
Treated plants and untreated controls were maintained in a greenhouse for
approximately 14 to 21 days, after which all treated plants were compared to
untreated
controls and visually evaluated. Plant response ratings, summarized in Table
C, were based
upon a 0 to 100 scale where 0 was no effect and 100 was complete control. A
dash response
(-) means no test result.
Table C COMPOUND
Rate 1120 g/ha 80 93 94 103 107 109 113 116 117 131 132 138 146 242
Postemergence
Arrowleaf sida 30 60 80 - 85 95 95 90 50 60 80 70 90 90
Barnyardgrass 20 95 65 80 95 95 95 90 90 95 95 85 95 95
Cocklebur 50 - - 0 - - 50 50 0 10 0 0 70 20
Common ragweed 5 20 5 5 50 20 20 0 50 0 0 - 30 80
Corn 0 45 0 0 60 55 60 20 85 40 10 60 50 20
Cotton 40 85 80 80 90 70 80 - 60 65 40 70 70 70
E. blacknightsh 60 85 95 0 95 95 95 50 80 80 0 70 85 90
Fall panicum 10 90 70 30 85 95 85 90 80 90 50 90 90 90
Field bindweed 0 50 0 0 60 10 50 50 40 60 70 50 0 0
Giant foxtail 20 95 40 40 95 85 80 85 80 80 0 85 85 85
H. beggarticks 10 70 20 5 95 85 50 - 0 70 - 80 85 90
I. morningglory 50 70 - 10 95 70 50 20 0 50 0 0 50 0
Johnsongrass 0 90 0 0 90 95 95 80 85 70 60 90 90 90
Ladysthumb 70 - 90 10 - 95 85 - - - - - - -
Lambsquarters 20 40 30 20 40 70 50 0 0 0 0 20 50 0
Large crabgrass 10 95 - 10 95 90 95 90 80 85 80 85 80 85
Purple nutsedge 0 10 0 0 10 0 10 10 80 80 0 70 0 80
Redroot pigweed 80 85 0 85 80 85 90 20 30 30 30 70 20 50
Soybean - 85 55 35 85 85 85 40 60 45 40 40 85 65
Surinam grass 10 85 10 5 95 95 90 90 90 90 30 90 95 90
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Velvetleaf 20 70 40 45 75 75 75 80 60 70 0 80 60 60
Wild poinsettia 5 70 85 60 80 90 95 - 0 80 0 70 70 85
Table C COMPOUND
Rate 560 g/ha 80 93 94 103 107 109 113 116 117 131 132 138 146 242
Postemergence
Arrowleaf sida - 60 80 0 75 85 70 85 0 30 10 - 85 70
Barnyardgrass 20 90 30 10 90 85 85 90 90 95 80 85 85 90
Cocklebur 50 40 - 0 - 60 50 0 0 0 0 0 70 0
Common ragweed 5 10 5 0 50 10 - 0 20 0 0 0 30 80
Corn 0 0 0 0 55 5 45 15 40 5 0 50 5 0
Cotton 40 70 70 40 80 70 50 50 30 40 20 40 65 45
E. blacknightsh 50 - 75 0 70 - - 10 70 50 0 70 85 60
Fall panicum 0 90 10 0 85 80 85 85 40 90 50 60 90 90
Field bindweed 0 0 0 0 30 10 50 50 30 0 40 0 0 0
Giant foxtail 0 80 10 0 95 80 80 60 75 60 0 80 80 80
H. beggarticks 10 5 5 0 70 70 30 90 - 40 - - 85 -
I. morningglory 30 10 90 0 30 50 50 0 0 20 0 0 20 0
Johnsongrass 0 85 0 0 90 60 60 60 40 60 0 60 60 60
Ladysthumb 70 80 85 10 30 30 85 - - - - - 85 -
Lambsquarters 20 10 10 5 40 30 20 0 0 - 0 10 10 0
Large crabgrass 10 50 70 0 95 90 95 30 60 70 40 85 60 85
Purple nutsedge 0 0 0 0 10 0 0 10 10 0 0 50 0 10
Redroot pigweed 50 10 0 70 80 70 0 0 0 20 - 40 - 10
Soybean 60 80 30 35 85 85 85 30 40 30 30 30 60 25
Surinam grass 0 50 0 0 80 50 90 - 40 85 0 85 50 85
Velvetleaf 20 40 20 10 70 50 60 40 20 10 0 70 40 40
Wild poinsettia 5 30 60 10 40 50 80 0 0 30 0 0 50 0
Table C COMPOUND
Rate 280 g/ha 80 93 94 103 107 109 113 116 117 131 132 138 146 242
Postemergence
Arrowleaf sida 5 10 10 0 30 70 40 - 0 10 0 - 45 30
Barnyardgrass 10 90 0 0 85 85 80 85 80 70 50 70 80 85
Cocklebur 10 35 0 0 50 30 50 - 0 0 0 0 40 0
Common ragweed 0 10 0 0 50 10 5 0 0 0 0 0 - 10
Corn 0 0 0 0 5 0 40 0 0 0 0 20 0 0
Cotton 35 30 70 20 60 50 15 50 10 10 10 30 65 20
E. blacknightsh 5 40 40 0 50 80 50 0 0 10 0 10 30 40
Fall panicum 0 80 0 0 60 50 80 60 - 40 30 0 60 85
Field bindweed 0 0 0 0 0 0 0 0 30 0 0 0 0 -
Giant foxtail 0 55 0 0 70 80 70 60 60 40 0 15 40 60
H. beggarticks - 0 0 0 60 5 30 - - - 0 10 20 -
I. morningglory 10 10 10 0 30 50 50 0 0 0 0 0 20 0
Johnsongrass 0 5 0 0 50 10 20 40 35 40 0 20 30 45
Ladysthumb 10 0 10 0 - 10 0 - - - - - 10 -
Lambsquarters 15 10 5 5 0 10 - - 0 0 0 0 5 0
Large crabgrass 0 30 0 0 85 60 85 0 20 20 10 10 60 30
Purple nutsedge 0 0 0 0 0 0 10 0 0 0 0 0 0 0
Redroot pigweed 0 - - 60 75 40 0 0 0 10 10 10 - 0
Soybean 20 60 15 30 70 70 70 10 35 25 20 30 50 25
Surinam grass 0 45 0 0 70 5 40 0 0 80 0 40 5 40
Velvetleaf 5 5 5 5 60 20 0 0 - 0 0 60 40 0
Wild poinsettia 0 0 0 0 15 30 50 0 0 10 0 0 40 0
Table C COMPOUND
Rate 140 g/ha 80 93 94 103 107 109 113 116 117 131 132 138 146 242
Postemergence
Arrowleaf sida 0 - - 0 - 60 30 0 0 - 0 0 40 10
Barnyardgrass 0 70 0 0 70 60 80 55 70 70 50 40 60 80
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Cocklebur 5 0 0 0 0 30 5 0 0 0 0 0 40
0
Common ragweed0 5 0 0 0 5 5 0 0 0 0 0 10
0
Corn 0 0 0 0 0 0 0 0 0 0 0 - 0 0
Cotton 20 15 20 0 45 10 10 10 5 10 5 5 40
0
E. blacknightsh0 10 0 0 50 50 50 0 0 0 0 0 0 0
Fall panicum 0 0 0 0 50 50 60 10 0 0 0 0 50
30
Field bindweed0 0 0 0 0 0 0 0 0 0 0 0 0 0
Giant foxtail 0 10 0 0 - 50 20 - 0 10 0 0 0 40
H. beggarticks0 - 0 0 5 - 5 80 - 0 0 - 10
-
I, morningglory0 5 0 0 10 0 10 0 0 0 0 0 0 0
Johnsongrass 0 0 0 0 35 0 0 10 10 15 0 0 0 45
Ladysthumb 10 0 5 0 0 - 0 - - - - - 0 -
Lambsquarters 0 10 0 0 0 10 0 0 0 0 0 0 0 0
Large crabgrass0 0 0 0 70 10 0 0 0 0 0 0 0 10
Purple nutsedge0 0 0 0 0 0 0 0 0 0 0 0 0 0
Redroot pigweed- 5 - 0 - 0 0 0 0 10 0 0 0 0
Soybean 5 40 15 30 45 35 40 10 10 20 5 10 40
20
Surinam grass 0 0 0 0 10 0 0 0 0 0 0 10 0 0
Velvetleaf 5 0 5 0 5 10 0 0 0 0 0 0 0 0
Wild poinsettia0 0 0 0 0 10 10 0 0 0 0 0 0 0
TEST D
Seeds, tubers, or plant parts of Alexandergrass (Brachiaria plantaginea),
bermuda-
grass (Cynodon dactylon), common purslane (Portulaca oleracea), common ragweed
(Ambrosia elation), common groundsel (Senecio vulgaris), dallisgrass (Paspalum
dilatatum),
goosegrass (Eleusine indica), guineagrass (Panicum maximum), itchgrass
(Rottboellia
exaltata), Johnson grass (Sorghum halepense), large crabgrass (Digitaria
sanguinalis), pitted
morningglory (Ipomoea lacunosa), purple nutsedge (Cyperus rotundas), sandbar
(Cenchrus
echinatus), sourgrass (Trichachne insularis), Spanishneedles (Bidens
bipinnata), surinam
grass (Brachiaria decumbens) and tall mallow (Malva sylvestris) were planted
into green-
house pots of flats containing greenhouse planting medium. Plant species were
grown in
separate pots or individual compartments. Preemergence applications were made
within one
day of planting the seed or plant part.
Test chemicals were formulated in a non-phytotoxic solvent mixture which
included a
surfactant and applied preemergence to the surface of the pot containing seeds
in a sandy
loam soil. Untreated control pots and treated pots were placed in the
greenhouse for growth
and visually evaluated for injury 14 to 21 days after herbicide application.
Plant response
ratings, summarized in Table C, are based on a 0 to 100 scale where 0 is no
injury and 100 is
complete control. A dash (-) response means no test result.
Table D COMPOUND Table D COMPOUND
Rate 500 g/ha 146 147 299 Itchgrass 65 65 100
Postemergence Johnsongrass 65 70 100
Alexandergrass 65 75 100 Large crabgrass 65 60 100
Bermudagrass 35 40 100 P. morninglory 65 30 0
C. purslane 20 10 0 Purple nutsedge 35 60 100
C. ragweed 40 0 100 Sandbar 80 90 100
Com. groundsel 0 0 100 Sourgrass 80 80 -
Dallisgrass 80 85 100 Spanishneedles 20 20 100
Goosegrass 80 65 100 Surinam grass 80 70 100
Green foxtail - - 100 Tall Mallow 50 20 100
Guineagrass 60 60 100
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CA 02359108 2001-07-18
WO 00/43377 PCT/US00/01283
330
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CA 02359108 2001-07-18
WO 00/43377 PCT/US00/01283
331
TEST E
Compounds evaluated in this test were formulated in a non-phytotoxic solvent
mixture
which included a surfactant and applied to plants that were in the 1- to 4-
leaf stage
(postemergence application). A mixture of sandy loam soil and greenhouse
potting mix in a
60:40 ratio was used for the postemergence test.
Plantings of these crops and weed species were adjusted to produce plants of
appropriate size for the postemergence test. All plant species were grown
using normal
greenhouse practices. Crop and weed species include annual bluegrass (Poa
annua),
blackgrass (Alopecurus myosuroides), black nightshade (Solanum nigra),
chickweed
(Stellaria media), common poppy (Papaver rhoeas), deadnettle (Lamium
amplexicaule),
downy brome (Bromus tectorum), field violet (Viola arvensis), galium (Galium
aparine),
green foxtail (Setaria viridis), Italian ryegrass (Lolium multiflorum),
jointed goatgrass
(Aegilops cylindrica), kochia (Kochia scoparia), lambsquarters (Chenopodium
album),
littleseed canarygrass (Phalaris minor), rape (Brassica napus), redroot
pigweed
(Amaranthus retroJlexus), Russian thistle (Salsola kali), scentless chamomile
(Matricaria
inodora), spring barley (Hordeum vulgare), sugar beet (Beta vulgaris),
sunflower
(Helianthus annuus), ivyleaf speedwell (Veronica hederaefolia), spring wheat
(Triticum
aestivum), winter wheat (Triticum aestivum), wild buckwheat (Polygonum
convolvulus),
wild mustard (Sinapis arvensis), wild oat (Avena fatua), windgrass (Apera
spica-venti) and
winter barley (Hordeum vulgare).
Treated plants and untreated controls were maintained in a greenhouse for
approximately 21 to 28 days, after which all treated plants were compared to
untreated
controls and visually evaluated. Plant response ratings, summarized in Table
E, are based
upon a 0 to 100 scale where 0 is no effect and 100 is complete control. A dash
response (-)
means no test result.
CA 02359108 2001-07-18
WO 00/43377 PCT/US00/01283
332
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CA 02359108 2001-07-18
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Test F Protocol
Abutilon theophrasti (ABUTH), Chenopodium album (CHEAL), Amaranthus rudis
(AMATA), Setaria faberii (SETFA), Panicum dichotomiflorum (PANDI), and
Digitaria
sanguinalis (DIGSA) were grown from seed in pots of an artificial potting
mixture in a
greenhouse. Compounds of the present invention were applied at 70 and 105 g
ai/ha
preemergence. Rimsulfuron was applied at 8.8 and 17.5 g ai/ha. Mixtures of the
compounds
of the present invention and rimsulfuron were also applied.
Following application, the plants were maintained by watering as needed. A
fertilizer
solution of Peter's 20-20-20 ( 10 pounds/5 gallons of water) plus Sprint 330,
a Iron Chelate
micronutrient, (113.5 grams/5 gallons of water) was injected into the water
with an
Anderson fertilizer injection system to provide approximately 218 ppm of
nitrogen with each
watering. Artificial lighting was used to supplement natural light to produce
a 14 hour
photoperiod and an additional one hour light period was used between 1:00 am
to 2:00 am
1 S for a night interruption. Greenhouse temperatures were targeted for 27
°C in the day and 21
°C at night. At 21 days after treatment, all plants were evaluated for
injury as compared to
control plants that were sprayed only with non-phytotoxic solvent. Mean plant
response
ratings, summarized in Table F, are based upon a 0 to 100 scale where 0 is no
effect and 100
is complete control.
Colby's equation was used to calculate the expected additive herbicidal effect
of the
mixtures of Compound 21 and the mixture partners listed above. Colby's
equation (Colby,
S. R. "Calculating Synergistic and Antagonistic Responses of Herbicide
Combinations,"
Weeds, 15( 1 ), pp 20-22 ( 1967)) calculates the expected additive effect of
herbicidal
mixtures, and for two active ingredients is of the form:
Pa+b - Pa + Pb - (PaPb / 100)
wherein Pa+b is the percentage effect of the mixture expected from additive
contribution of the individual components,
Pa is the observed percentage effect of the first active ingredient at the
same
use rate as in the mixture, and
Pb is the observed percentage effect of the second active ingredient at the
same use
rate as in the mixture.
Combinations of Compound 113, Compound 131, and Compound 242 with
rimsulfuron are surprisingly found to provide better control of certain weeds
than expected
by calculation from the Colby's equation, thus demonstrating synergism. Weeds
other than
those specifically listed are also controlled by mixtures of compounds of the
present
invention and rimsulfuron. Different ratios of compounds of the present
invention with
rimsulfuron, and different formulation types, also provide useful weed control
from the
combination of the two herbicides.
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TABLE F
ABUTH CHEAL
Cmpd. 113 RimsulfuronObservedExpected Observed Expected
fi
Alone
70 0 45 - 15 -
105 0 65 - 35 -
0 8.8 20 - 25 -
0 17.5 40 - 60 -
Mixtures
70 8.8 75 56 60 36
70 17.5 85 67 95 66
105 8.8 90 72 100 51
105 17.5 80 79 100 74
AMATA SETFA
Cmpd.113RimsulfuronObserved ExpectedfiObserved Expectedfi
Alone
70 0 35 - 60 -
105 0 25 - 65 -
0 8.8 10 - 75 -
0 17.5 15 - 90 -
Mixtures
70 8.8 15 23 95 90
70 17.5 70 45 100 96
105 8.8 25 33 100 91
105 17.5 90 36 100 97
PANDI DIGSA
Cmpd. RimsulfuronObserved Expected Observed Expected-
113 j~
Alone
70 0 100 - 95 -
105 0 95 - 70 -
0 8.8 75 - 95 -
0 17.5 95 - 100 -
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Mixtures
70 8.8 90 100 100 100
70 17.5 100 100 100 100
105 8.8 100 99 90 99
105 17.5 85 99 100 100
ABUTH CHEAL
Cmpd. RimsulfuronObserved Expected- Observed Expected
131 fi
Alone
70 0 40 - 60 -
105 0 60 - 95 -
0 8.8 20 - 25 -
0 17.5 40 - 60 -
Mixtures
70 8.8 50 52 95 70
70 17.5 85 64 100 84
105 8.8 80 68 95 96
105 17.5 75 76 100 98
AMATA SETFA
Cmpd.131 RimsulfuronObserved ExpectedtObserved Expectedfi
Alone
70 0 50 - 35 -
105 0 40 - 65 -
0 8.8 10 - 75 -
0 17.5 15 - 90 -
Mixtures
70 8.8 95 54 85 84
70 17.5 100 58 100 93
105 8.8 95 46 95 91
105 17.5 85 49 100 97
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PANDI DIGSA
Cmpd. RimsulfuronObserved Expectedt Observed Expected-
131
Alone
70 0 100 - 100 -
105 0 95 - 100 -
0 8.8 75 - 95 -
0 17.5 95 - 100 -
Mixtures
70 8.8 75 100 100 100
70 17.5 95 100 100 100
105 8.8 100 99 100 100
105 17.5 100 100 100 100
ABUTH CHEAL
Cmpd. RimsulfuronObserved Expected Observed Expected
242 f
Alone
70 0 50 - 30 -
105 0 70 - 100 -
0 8.8 20 - 25 -
0 17.5 40 - 60 -
Mixtures
70 8.8 85 60 100 48
70 17.5 80 81 85 72
105 8.8 85 76 100 100
105 17.5 80 82 100 100
AMATA SETFA
Cmpd. RimsulfuronObserved Expected Observed Expected
242 fi fi
Alone
70 0 20 - 60 -
105 0 55 - 75 -
0 8.8 10 - 75 -
0 17.5 15 - 90 -
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Mixtures
70 8.8 70 28 90 90
70 17.5 85 32 100 96
105 8.8 35 60 75 94
105 17.5 65 62 100 97
PANDI DIGSA
Cmpd. RimsulfuronObserved Expected Observed Expected-
242 f
Alone
70 0 60 - 100 -
105 0 80 - 100 -
0 8.8 75 - 95 -
0 17.5 95 - 100 -
Mixtures
70 8.8 95 90 100 100
70 17.5 100 98 100 100
105 8.8 100 85 100 100
105 17.5 100 99 100 100
* Data are reported as percent control.
Expected from the Colby Equation
S
Test G protocol
In soil-containing pots were planted seeds of maize hybrid P33G26 that was
previously
treated with dichlormid, fenchlorazole-ethyl, and naphthalic anhydride (or no
safener). The
soil surface was then treated with several rates of Compound 131 or Compound
146
dissolved in a non-phytotoxic solvent using a flat-fan sprayer calibrated to
deliver 310 L/ha.
Treatments were replicated 4 or 5 times. The treated and untreated plants were
allowed to
grow in a greenhouse using supplementary artificial lighting with a day-length
of 14 hours,
with the temperature maintained at about 27 °C during the day and 24
°C during the night.
Plants were kept watered with a dilute balanced fertilizer solution.
At 28 days after application, the treated plants were compared with untreated
controls
and visually evaluated. Mean plant response ratings, summarized in Table G,
are based
upon a 0 to 100 scale where 0 is no effect and 100 is complete control.
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TABLE G*
Safener
Compd Rate None DichlormidFenchlorazole-naphthalic
(g ai/ha) ethyl anhydride
131 560 95 40 96 ND~'
131 280 91 3 92 ND-~
131 140 88 3 91 0
131 70 80 3 85 ND~
146 1120 85 4 85 35
146 560 80 4 78 NDfi
146 280 73 1 74 ND~
146 140 49 1 3 0
* Data are reported as percent control.
naphthalic anhydride treatment severely inhibited corn germination. Where corn
S did satisfactorily emerge, it was safened against the herbicide damage.
As can be seen from Table F, in the absence of any safener, both Compound 131
and
Compound 146 at rates ranging from 70 to 560 g/ha, and 140 to 1120 g/ha
respectively, were
severely injurious to maize. With the exception of Compound 131 at the rate of
560 g/ha
(entry 1 in Table F), the presence of dichlormid reduced the injury to an
insignificant level
from which the corn would be expected to recover with no long-term deleterious
effects.
The presence of fenchlorazole-ethyl, however, did not provide safening effects
except for low
rate of Compound 146 (Entry 8 in Table F). The dramatic safening effects
observed here
were unexpected and surprising. Based on this discovery, it is anticipated
that other
compounds known to safen herbicides on corn, soybeans or other crops are
useful in
safening compounds of the present invention on corn, soybeans or other crops.
Test H protocol
Mixtures of the herbicide and safeners were applied to pots of a soil mixture
previously sown with corn. Pioneer hybrid P33G26 corn was sown in pots
containing a
sterile mix of 60% sassafras soil and 40% Metro Mix 360 ~ growing medium (pH
6.7, O.M.
2%). Test compounds were dissolved in AGWT (a mixture of 0.25% Tween 20
surfactant,
5% water, 5% glycerin and 89.75% acetone) and sprayed on the soil as pots
passed under a
stationary 8002E nozzle. Treatments were applied at a 33 gal/acre rate of the
AGWT carrier.
After treatment, the test pots were placed in the greenhouse and watered.
There were two
replications for each treatment. Each pot contained eight corn seeds. The pots
within each
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replication were placed in random positions on greenhouse benches. Test plants
were
fertilized as they were watered with approximately 200 ppm of N (as water
soluble 20-20-20
fertilizer) which was metered into the water lines with a fertilizer injector.
Daytime
temperature was 23-30 C° and night time temperature was 18-25
C°. The test plants were
S supplemented with artificial lighting. The lights were activated whenever
the natural light
intensity dropped below the programmed threshold. Day length was maintained
for
approximately 14 hours.
The test was evaluated approximately 12 days after treatment. Treated plants
were
visually compared to untreated controls and rated on a scale from 0 to 100
where 0 is no
effect and 100 is plant death. The results summarized in Table H are the
averages from the
two replications for each treatment.
TABLE H
Compd Rate None DichlormidDichlormidDichlormid
(g ai/ha) 70 g/ha 140 g/ha 280 g/ha
113 70 18 0 0 0
113 140 25 20 0 0
113 280 53 35 28 33
Compd Rate None BenoxacorBenoxacor Benoxacor
(g ai/ha) 70 g/ha 140 g/ha 280 g/ha
113 70 18 0 0 0
113 140 25 0 0 8
113 280 53 38 18 20
As shown in Table H, both dichlormid and benoxacor functioned very effectively
as
safeners for Compound 113. Without safener, Compound 113 at rates from 70 to
280 g/ha
produced corn injury of 18 to 53%. In the presence of dichlormid or benoxacor
at rates from
70 to 280 g/ha, corn injury was reduced to from 0 to 38%. The dramatic and
unexpected
safening by dichlormid and benoxacor demonstrates the potential utility of
mixtures of these
compounds with Compound 113, or other similar compounds of this invention, for
the
control of undesired vegetation in corn production.
