Process for the preparation of optically active...

C - Chemistry – Metallurgy – 07 – D

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C07D 241/06 (2006.01) C07D 241/04 (2006.01) B01J 31/22 (2006.01) B01J 31/28 (2006.01)

Patent

CA 2177227

Optically active piperazine-2-carboxylic acid derivatives of the general formula: Image wherein R1 and R2 are inter alia hydrogen, alkyl or acyl and X is hydroxyl, alkoxy or a (substituted) amino group, are prepared by asymmetric hydrogenation of the corresponding 1,4,5,6-tetrahydropyrazines, catalyzed by optically active rhodium, ruthenium or iridium complexes. The compounds of the formula I are intermediates for the preparation of pharmaceutically active ingredients, for example HIV protease inhibitors.

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