ONE-POT PREPARATION OF CYCLOBENZAPRINE HYDROCHLORIDE

摘要

Disclosed herein is a one-pot process for the preparation of pharmaceutically active cyclobenzaprine hydrochloride (Formula I) which comprises, reacting 5-dibenzosuberenone with Grignard reagent derived from 3-dimethylaminopropyl chloride. The reaction mass undergoes hydrolysis and dehydration reaction without isolation of intermediate compound in presence of aq. HCl solution. After completion of the reaction, the reaction mass is neutralized and the product is extracted in an organic solvent which is further converted to its hydrochloride salt. The method has the advantages of compact preparation process, low cost, high yield and suitability for large scale industrialized production.