Regio- and Enantioselective Synthesis of alpha-Amino-delta-Ketoesters Through Catalytic Umpolung Reaction of alpha-Iminoesters with Enones

Chiral alpha-amino-delta-keto esters are important precursors of organocatalysts, pharmaceuticals, and biochemically interesting molecules. The organocatalytic asymmetric umpolung reaction of imines has been developed to obtain chiral amines in a highly enantioselective manner. Herein, we report the organocatalytic asymmetric umpolung synthesis of alpha-amino-delta-keto esters in high yield (up to 95% ee, >20/1 r.r.).