Patent ID: 7705163
Filing Date: 2010-04-27
Classification: A61P,C07D

Abstract:
1. A process for the preparation of carvedilol of formula (I): either in enantiomerically pure form, or as an enantiomeric mixture, optionally as a pharmaceutically acceptable salt thereof, which process comprises reacting 2,3-epoxypropoxy carbazole of formula (II): in the form of the R or S enantiomer, or a mixture thereof, with N-[2-(2-methoxyphenoxy)ethyl]-benzylamine of formula (V): to yield benzyl carvedilol of formula (VI): which is debenzylated by catalytic hydrogenation to yield carvedilol of formula (I), either in enantiomerically pure form, or as an enantiomeric mixture, and if desired reacting the thus formed carvedilol of formula (I) with an inorganic or organic acid to yield a pharmaceutically acceptable salt thereof, and/or, if desired, separating the enantiomers; which process is characterized in that reaction of said 2,3-epoxypropoxy carbazole of formula (II) with said N-[2-(2-methoxy-phenoxy)ethyl]-benzylamine of formula (V) is carried out in water as the reaction medium and in the absence of an organic solvent.