Asymmetric S‐Michael Reaction: Synthesis of CF₂H−Containing S‐Ether Compounds through Isosteric Replacement

Abstract

Optical pharmaceutical important compounds which bring CF 2 H to mimic the role of -SH were synthesized through the asymmetric S-Michael addition reaction in the presence of quinine-a derived squaramide catalyst. Various sulfhydryl compounds including Benzyl mercaptan, phenthiol, alkyl thio-phenol, mercaptoacetate, methyl 3-mercaptoacrylate, and 1,4dithiane-2,5-diol were tested. The broad substrate scope, good functional group tolerance, and easy derivatization make this synthesis method very attractive.