Catalytic enantioselective electrophilic α-amination of β-ketoesters catalyzed by chiral palladium complexes

The catalytic enantioselective electrophilic α-amination promoted chiral palladium complexes is described. Treatment of β-ketoesters with azodicarboxylates as electrophilic amination reagents under mild reaction conditions afforded the corresponding α-amino β-ketoesters with excellent enantiomeric excesses (91–99% ee). Palladium complexes were immobilized in [bmim]PF6, and their applications to catalytic α-amination of β-ketoesters were successfully demonstrated.