NOVEL SYNTHESIS PROCESS OF (2E)-3-(3,4-DIMETHOXYPHENYL) PROP-2-ENENITRILE, AND APPLICATION IN THE SYNTHESIS OF IVABRADINE AND ADDITION SALT THEREOF WITH PHARMACEUTICALLY ACCEPTABLE ACID

摘要

PROBLEM TO BE SOLVED: To provide a production method of an intermediate in the synthesis of ivabradine, salts thereof with a pharmaceutically acceptable acid and hydrates thereof.SOLUTION: A synthesis process gains (2E)-3-(3,4-dimethoxy) prop-2-enenitrile shown in formula (I) which is an intermediate of ivabradine synthesis that is useful for treatment of heart disease, by making a compound shown in formula (IX) coupling react with acrylonitrile in an organic solvent under presence of palladium catalyst, ligand, base and phase transfer agent.SELECTED DRAWING: None