Enantioselective Formal C-H Conjugate Addition of Acetanilides to b-Substituted Acrylates by Chiral Iridium Catalysts

摘要

The Ir-catalyzed enantioselective reaction of substituted acetanilides with b-substituted a,b-unsaturated esters provided chiral 3,3-disubstituted propanoates in high yield with good-to-excellent enantiomeric excess (up to 99% ee). This transformation, initiated by sp2 C-H bond activation, is the first example of enantioselective formal C-H conjugate addition to b-substituted a,b-unsaturated carbonyl compounds. The starting materials are commercially available and/or readily accessible.