NOVEL PROCESS FOR THE SYNTHESIS OF 1,3,4,5-TETRAHYDRO-2H-3-BENZAZEPIN-2-ONE DERIVATIVES AND THE APPLICATION TO THE SYNTHESIS OF IVABRADINE AND ITS SALTS OF ADDITION TO A PHARMACEUTICALLY ACCEPTABLE ACID

摘要

Preparation of N-substituted tetrahydro-3-benzazepine derivatives (I) by catalytic hydrogenation of the corresponding dihydro compound (VI) at 40-80[deg]C, then filtering and crystallizing the product. Preparation of N-substituted 3-benzazepine derivatives of formula (I) by catalytic hydrogention of the corresponding dihydro compound of formula (VI) at 40-80[deg]C, then filtering and crystallizing the product. R 1 and R 21-6C linear or branched alkoxy or together complete a 1,3-dioxan or 1,3-dioxolan ring Independent claims are also included for the following: (1) (I) as new compounds; and (2) method for synthesis of ivabradine or its pharmaceutically acceptable salts from (I). [Image].