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Details for Patent: 5,352,795

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Details for Patent: 5,352,795

Title: Alpha-heterocycle substituted tolunitriles
Abstract:The invention is concerned with aromatase inhibiting compounds of formula I ##STR1## wherein R and Ro represent hydrogen or lower alkyl; or R and Ro located on adjacent carbon atoms and together when combined with the benzene ring to which they are attached form a naphthalene or tetrahydronaphthalene ring; R.sub.1 and R.sub.2 independently represent hydrogen, lower alkyl, (lower alkyl, aryl or aryl-lower alkyl)-thio, lower alkenyl, aryl, aryl-lower alkyl, C.sub.3 -C.sub.6 -cycloalkyl, or C.sub.3 -C.sub.6 -cycloalkyl-lower alkyl; or R.sub.1 and R.sub.2 combined represent lower alkylidene, mono-or di-aryl-lower alkylidene; R.sub.1 and R.sub.2 combined also represent C.sub.4 -C.sub.6 -straight chain alkylene, lower alkyl-substituted straight chain alkylene or ortho-phenylene bridged-C.sub.2 -C.sub.4 -straight chain alkylene, each forming with the carbon atom attached thereto a corresponding optionally substituted or benzo-fused 5, 6 or 7-membered ring; W represents 1-imidazolyl, 1-(1,2,4- or 1,3,4)-triazolyl or 3-pyridyl; or W represents 1-imidazolyl, 1-( 1,2,4 or 1,3,4)-triazolyl or 3-pyridyl substituted by lower alkyl; and pharmaceutically acceptable salts thereof.
Inventor(s): Bowman; Robert M. (Summit, NJ), Browne; Leslie J. (Morristown, NJ)
Assignee: Ciba-Geigy Corporation (Ardsley, NY)
Filing Date:May 11, 1992
Application Number:07/882,188
Claims:1. A method for preparing a compound of the formula ##STR16## wherein R and R.sub.o represent hydrogen or lower alkyl; or R and R.sub.o located on adjacent carbon atoms and together when combined with the benzene ring to which they are attached form a naphthalene or tetrahydronaphthalene ting; R.sub.1 represents hydrogen; R.sub.2 represents 4-cyanophenyl; and W represents 1-(1,2,4)-triazolyl; which comprises condensing under basic conditions using an alkali metal aikoxide a compound of the formula XI ##STR17## wherein R, R.sub.o and W have meaning as defined above, with p-fluorobenzonitrile.

2. A method according to claim 1 wherein the alkali metal alkoxide is potassium t-butoxide.

3. A method according to claim 1 for preparing 4-[alpha-(4-cyanophenyl)-1-(1,2,4-triazolyl)-methyl]benzonitrile which comprises condensing 4-[1-(1,2,4)-triazolylmethyl]benzonitrile with 4-fluorobenzonitrile using potassium tert-butoxide in dimethylformamide.

4. A process according to claim 1 for preparing 4-[alpha-(4-cyanophenyl)-1-(1,2,4-triazolyl)-methyl]benzonitrile.
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