| abstract |
The present invention provides a novel synthesis process of a compound (2E) -3- (3,4-dimethoxyphenyl) -2-enenitrile represented by the formula (I). The compound is an intermediate in the synthesis of ivabradine, its addition salt with a pharmaceutically acceptable acid and its hydrate. Synthesis in which a compound of formula (IX) undergoes a coupling reaction with acrylonitrile in an organic solvent in the presence of a palladium catalyst, a ligand, a base and a phase transfer agent. process. The palladium catalyst is palladium carbon, the ligand is tri (o-tolyl) phosphine, the base is sodium acetate, the phase transfer agent is tetrabutylacetamide bromide, and the organic solvent is N- Synthesis process of formula (1), which is dimethylacetamide. [Selection figure] None |