Mild Enantiopure Synthesis of α-Amino Ketones from Thiol Esters

Significance

Herein, the authors describe a novel efficient synthesis of enantiopure N-protected α-amino ketones starting from chiral thiol esters. This Pd-catalyzed, copper diphenylphosphinate mediated reaction proceeds under mild and pH-neutral conditions and gives the amino ketones in high yields and very high enantiopurity.