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) A61H 23/00 (2006.01)

Patent

CA 1098540

ABSTRACT OF THE DISCLOSURE A process is disclosed for the resolution of racemic .alpha.- aminonitriles of the formula Image (I) wherein R1 is hydrogen or methyl, R2 is hydrogen or methoxy and R3 is hydrogen or methyl,wherein the racemic mixture is reacted with (-)-mandelic acid in alkanol/C5-8 hydrocarbons to obtain a racemic mixture of diastereo- isomeric D and L salts of (-)-mandelic acid, which mixture is then macerated with alkanol/C5-8 hydrocarbon system to dissolve the L salt and the D-salt is filtered off. The D-salt is racemized with ammonia and the D.L-amino- nitrile recycled. The L-salt is neutralized and the L-aminonitrile extracted and converted into a stable form such as the hydrochloride or acyl derivative.

300404

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