Patent ID: 8278440
Filing Date: 2012-10-02
Classification: A61P,C07C,C07D

Abstract:
1. A process for the synthesis of ivabradine of formula (I): wherein a compound of formula (VI): is subjected to the action of a thiol in an organic solvent to form a hemithioacetal of formula (VII): wherein R represents a substituted or unsubstituted, optionally perfluorinated, linear or branched alkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted benzyl group or a CH which is subjected to a cyclisation reaction to yield a compound of formula (VIII): wherein R is as defined hereinbefore, which is subjected to a reduction reaction to yield ivabradine of formula (I), which may optionally be converted into an addition salt thereof with a pharmaceutically acceptable acid selected from hydrochloric acid, hydrobromic acid, sulphuric acid, phosphoric acid, acetic acid, trifluoroacetic acid, lactic acid, pyruvic acid, malonic acid, succinic acid, glutaric acid, fumaric acid, tartaric acid, maleic acid, citric acid, ascorbic acid, oxalic acid, methanesulphonic acid, benzenesulphonic acid and camphoric acid, and into hydrates thereof.