RAPID AND EFFICIENT ACCESS TO MESO-2,5-CIS-DISUBSTITUTED PYRROLIDINES BY DOUBLE AZA-MICHAEL REACTIONS OF CHIRAL PRIMARY AMINES

摘要

The double aza-Michael reaction of enantiopure primary amines on bis alpha,beta-unsaturated diesters has been studied under various activating conditions.High pressure allowed a rapid and efficient access to meso-2,5-disubstituted pyrrolidines.2,5-Disubstituted pyrrolidines are naturally ubiquitous,biologically important substances and the synthesis of this type of alkaloids is of considerable current interest.