摘要

An efficient catalytic asymmetric three-component sulfa-Michael/aldol cascade reaction has been developed using a chiral multi-functional catalyst. This reaction provided facile access to gamma-sulfur-beta-nitro-alpha-hydroxy esters bearing three consecutive linear stereocenters in high yields (up to 97%) with excellent diastereo- (up to >97:3 dr) and enantioselectivities (>99% ee). These compounds were readily converted into 2-nitroallylic alcohols and potentially bioactive gamma-sulfur-beta-amino-alpha-hydroxy esters, which could be further used for the synthesis of Bestatin derivatives.