A procedure for the synthesis of (1H) - 4.5 - Dimethoxy - 1 - (benzo - ciclobutano metilaminometil) - and their Addition salts, a method for the resolution of Racemic Synthesis Intermediate and its application to the synthesis of Ivabradine and its Addition salts with a pharmaceutically acceptable acid

摘要

Claim 1: procedure for resolution of the Amine of formula (1), by reaction with a diacidic optically Active Compound, followed by Filtration and Filtration with Suction, the suspension so obtained for the compound of formula (2), which is reacted with a base, PA Ra obtain corresponding Amine of formula (3), configuration (S).Claim 1: procedure for Synthesis of the compound of formula (4), configuration (S) from the compound of formula (5), which is reduced to obtain the Racemic Amine of formula (1), which is resolved according to the procedure of any one of claims 1 to 10, P To give the optically Active Amine of formula (3),That is reacted with Ethyl chloroformate, to give the optically Active Compound of formula (6), which reduces its carbamate function to obtain the compound of formula (4).Claim 1: procedure for the synthesis of Ivabradine and its pharmaceutically acceptable salts, hydrates, wherein the compound of formula (5) is the intermediate Compound of formula (4) According to the procedure of claim 11, and then the compu This intermediate of formula (4) becomes Ivabradine.