The enantioselective synthesis of (S)-(+)-mianserin and (S)-(+)-epinastine

Beilstein J Org Chem. 2015 Aug 28:11:1509-13. doi: 10.3762/bjoc.11.164. eCollection 2015.

Abstract

A simple enantioselective synthetic procedure for the preparation of mianserin and epinastine in optically pure form is described. The key step in the synthetic pathway is the asymmetric reduction of the cyclic imine using asymmetric transfer hydrogenation conditions.

Keywords: chiral diamines; enantioselective reduction; epinastine; mianserin; ruthenium complexes.