Process for preparation of Rasagiline and salts thereof

摘要

The present invention relates to an improved process for the preparation of Rasagiline or pharmaceutically acceptable salts thereof. The present invention also relates to Rasagiline salts, polymorphs thereof and process for preparation thereof.

主权项

1. A process for preparation of R(+)-Rasagiline or pharmaceutically acceptable salt thereof comprising,
a) reacting R(−)-1-aminoindan or a salt thereof with propargyl benzenesulfonate in aqueous medium at a temperature of 10-30° C. for about 2 to 4 hours in the presence of a base and a phase transfer catalyst to obtain a reaction mixture comprising R(+)-Rasagiline; b) optionally isolating R(+)-Rasagiline and/or unreacted R(−)-1-aminoindan from the reaction mixture; c) optionally converting R(+)-Rasagiline to pharmaceutically acceptable salt thereof.