Process for the synthesis of derivatives of 7,8-dimethoxy-1,3-dihydro-2H-3-benzazepin-2-one and its use for the preparation of ivabradine

摘要

Synthesis of dihydro-1H-benzo[d]azepine (I) involves subjecting 7,8-dimethoxy-2,3,4,5-tetrahydro-1H-3-benzazepine-2,4-dione (VII) to reduction reaction in presence of lithium triethylborohydride in an organic solvent. Synthesis of dihydro-1H-benzo[d]azepine of formula (I) involves subjecting 7,8-dimethoxy-2,3,4,5-tetrahydro-1H-3-benzazepine-2,4-dione of formula (VII) to reduction reaction in presence of lithium triethylborohydride in an organic solvent. R : p-methoxybenzyl or group of formula (i). Independent claims are included for the following: (1) 3-[3-({[(7S)-3,4-dimethoxybicyclo[4.2.0]octa-1(6),2,4-trien-7-yl]methyl}(methyl)amino)propyl]-7,8-dimethoxy-2,3,4,5-tetrahydro-1H-3-benzazepine-2,4-dione; and (2) 2-[2-({[3-({[(7S)-3,4-dimethoxybicyclo[4.2.0]octa-1(6),2,4-trien-7-yl]methyl}(methyl)amino)propyl]carbamoyl}methyl)-4,5-dimethoxyphenyl]acetic acid. [Image] ACTIVITY : Antianginal; Antiarrhythmic; Cardiant; Vasotropic.