Kinetic Resolution of α‐Hydroxyamide via N‐Heterocyclic Carbene‐Catalyzed Acylation

Abstract The effect of N‐substituent of α‐hydroxyamides on the performance of chiral N‐heterocyclic carbene‐catalyzed kinetic resolution was examined. N ‐ tert ‐Butyl‐α‐hydroxyamides provided the best performance and underwent enantioselective acylation with α‐bromo aldehyde by chiral N‐heterocyclic carbene/carboxylate anion co‐catalysis to realize kinetic resolution in high selectivity factor up to 128.