Facile Synthesis of Carvedilol from Corresponding N-Sulfonamide

B Anand Kumar, R Buchi Reddy,

Abstract

The synthesis of Carvedilol (1) was achieved from 2-(2-methoxyphenoxy)-N tosylethanamine (6) in a three steps. 2-(2-methoxyphenoxy)-N-tosylethanamine(6)1-(9H-carbazol-4-yloxy)-3-(N-(2-(2-methoxyphenoxy)ethyl)-N tosylamino)propan-2-ol (7) are intermediates. This1-(9H-carbazol-4-yloxy)-3-(N-(2-(2-methoxyphenoxy) ethyl)-N-tosylamino) propan-2-ol were conveniently desulfonylated with Mg in methanol. The followed synthetic sequence avoids/minimize the formation of impurity B (bis impurity). This approach could be useful for the preparation of pharmaceutically important moieties containing β-amino alcohols without formation of bis impurity.