Process for the synthesis of (2E)-3-(3,4-dimethoxyphenyl)prop-2-enenitrile, and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid

摘要

The invention relates to a process for the synthesis of (2E)-3-(3,4-dimethoxyphenyl)prop-2-enenitrile of formula (I):characterized in that the compound of formula (IX):is subjected to a coupling reaction with acrylonitrile in the presence of a palladium catalyst, a ligand, a base and a phase transfer agent in an organic solvent to yield the compound of formula (I).The invention relates also to a process for the synthesis of ivabradine, pharmaceutically acceptable salts thereof and hydrates thereof using the compound of formula (I). The said process provides a high percentage of the finished product yield.