Preparation of rasagiline and salts thereof
AssigneeDr. Reddy's Laboratories, Inc.
InventorsPraveen Cherukupally, Venkata Reddy Vajrala, Vijaya Kumar Adla, Srinivasulu Rangineni, Sundaralakshmi Kanniah
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Abstract
The present invention relates to processes for the preparation of rasagiline mesylate. Also provided is rasagiline mesylate having 90 volume percent of the particles (D90) with sizes less than about 6 μm and processes for the preparation thereof.
Claims15
A process for preparing rasagiline or a pharmaceutically acceptable salt thereof, comprising:
- (a) reacting 1-indanone of Formula II with propargylamine or a salt thereof, in the presence of a solvent, to afford N-(2-propynyl)-indanylimine of Formula III or a salt thereof, which is optionally isolated;
- and
- (b) reducing N-(2-propynyl)-indanylimine of Formula III or a salt thereof with a reducing agent, to afford a compound of Formula IV.
Rasagiline mesylate particles having a particle size distribution with D90 less than or equal to about 6 μm.
A process for preparing rasagiline mesylate particles having a particle size distribution with D90 less than or equal to about 6 μm, comprising:
- a) providing a solution of rasagiline mesylate in isopropyl alcohol;
- b) combining the rasagiline mesylate solution of a) with an anti-solvent;
- c) recovering solid rasagiline mesylate from b);
- and
- d) reducing particle sizes of rasagiline mesylate to obtain a particle size distribution with D90 less than about 6 μm.
A process for preparing rasagiline mesylate particles having D90 less than or equal to about 6 μm, comprising:
- a) slurrying rasagiline mesylate in an ether;
- b) recovering solid rasagiline mesylate from a), and
- c) reducing particle sizes of rasagiline mesylate to obtain D90 less than about 6 μm.
Dependencies are inferred from the claim text.