Method for racemisation of (s)-(+)- and...

Details Method for racemisation of (s)-(+)- and... Method for racemisation of (s)-(+)- and...

C - Chemistry, Metallurgy

07

D

C07D 223/28 (2006.01)

Patent

CA 2525419

A high-yielding method for racemisation of (S)-(+)- and (R)-(-)-10, 11- dihydro-l0-~hydroxy-5H-dibenz/b,f/azepine-5-carboxamide and a useful intermediate, 10-chloro-10, 11 dihydro-5H-dibenz/b,f/azepine-5-carboxamide (VII) are disclosed. Also disclosed are methods for the racemisation of optically pure or optically enriched mixtures of (S)-(+)-10,11-dihydro-l0- ~hydroxy-5H-dibenz/b,f/azepine-5-carboxamide (I) and (R)-(-)-10,11-dihydro-l0- hydroxy-5H-dibenz/b,f/azepine-5-carboxamide (II) to racemic (.plusmn.)-10,11- dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide (III).

L'invention porte sur un procédé à fort rendement de racémisation de (S)-(+)- et (R)-(-)-10, 11- dihydro-l0--hydroxy-5H-dibenz/b,f/azépine-5-carboxamide et sur un intermédiaire utile le 10-chloro-10, 11 dihydro-5H-dibenz/b,f/azépine-5-carboxamide (VII). L'invention porte également sur des procédés de racémisation de mélanges optiquement pures ou optiquement enrichis de (S)-(+)-10,11-dihydro-l0--hydroxy-5H-dibenz/b,f/azépine-5-carboxamide (I) et de (R)-(-)-10,11-dihydro-l0-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide (II) donnant du (.plusmn.)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azépine-5-carboxamide (III).

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