Process for the resolution of racemic alpha- aminonitriles

Details Process for the resolution of racemic alpha- aminonitriles Process for the resolution of racemic alpha- aminonitriles

A - Human Necessities

61

K

260/562.7

A61K 31/275 (2006.01)

Patent

CA 1098541

ABSTRACT OF THE DISCLOSURE A process is disclosed for the resolution of racemic .alpha.- aminonitriles of the formula Image (T) wherein R1 is hydrogen or methyl, R2 is hydrogen or methoxy and R3 is hydrogen or methyl, wherein the racemic mixture is reacted with (-)dibenzoyl-tartaric acid in a polar solvent to obtain a racemic mixture of diastereoisomeric D and L salts of (-)-dibenzoyl-tartaric acid. The racemic mixture of salts is macerated with aqueous dioxan to dissolve the D salt. The L salt is separated, neutralized and the L-amino nitrile extracted and converted into a stable form such as the hydrochloride or acyl derivative. The D salt is racemized with ammonia and the D,L-aminonitrile recycled.

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