NEW PROCESS FOR THE SYNTHESIS OF IVABRADINE AND ADDITION SALTS THEREOF WITH A PHARMACEUTICALLY ACCEPTABLE ACID

摘要

Synthesis of ivabradine involves subjecting 3-(7,8-dimethoxy-2-oxo-1,2,4,5-tetrahydro-benzo[d]azepin-3-yl)-propionaldehyde to a reductive amination reaction with ((S)-3,4-dimethoxy-bicyclo[4.2.0]octa-1,2,4-trien-7-ylmethyl)-methyl-amine in presence of formic acid (greater than 1 equivalent per equivalent of aldehyde) and of triethylamine (greater than 1 equivalent per equivalent of aldehyde), at 15-100[deg] C, in absence of solvent/alcoholic solvent. ACTIVITY : Cardiant; Antianginal; Cardiant; Cardiant. No biological data given.