PROCESS FOR THE PREPARATION OF RASAGILINE AND ITS SALTS

摘要

The present invention provides a novel process for the preparation of rasagiline or its salts, in particular rasagiline mesylate, which process comprises the steps of : (a) reacting racemic N-benzyl-1-indanamine with (R,R)-tartaric acid in water; (b) cooling the mixture of step (a) to form a salt of (R)-enantiomerically enriched N-benzyl-1-indanamine with (R,R)-tartaric acid in solid form; (c) separating said precipitated solid obtained in step (b); (d) hydrogenating under catalytic conditions the solid product of step (c), optionally, in the presence of acids, bases or salts; (e) basifying the reaction mixture of step (d) with aqueous base and isolating (R)-enantiomerically enriched 1-indanamine from the obtained mixture; and (f) converting the (R)-enantiomerically enriched 1-indanamine of step (e) to rasagiline or its salts.