NEW PROCESS FOR THE SYNTHESIS OF IVABRADINE AND ADDITION SALTS THEREOF WITH A PHARMACEUTICALLY ACCEPTABLE ACID.

摘要

Preparing ivabradine compounds (VI) comprises reacting 3,4-dimethoxy-bicyclo[4.2.0]octa-1,3,5-triene-7-carbaldehyde (VII) with an amine (VIII) in the presence of a reducing agent. Preparing ivabradine compounds of formula (VI) comprises reacting 3,4-dimethoxy-bicyclo[4.2.0]octa-1,3,5-triene-7-carbaldehyde of formula (VII) with an amine of formula (VIII) in the presence of a reducing agent. [Structures (VI)-(VIII), page 16] A : CH 2CH 2 or CH=CH. An independent claim is also included for (VII) in racemic or optically active form. - ACTIVITY : Cardiant; Antianginal; Antiarrhythmic. - MECHANISM OF ACTION : None given.