LAUSR

Abstract We report a novel and efficient Cu-catalyzed direct asymmetric amination of tertiary β-carbonyl compounds using aryl hydroxylamine as electrophilic nitrogen donor. The process facilitates the convenient and direct synthesis of chiral α-amino carbonyl derivatives, without the need for any post-reaction manipulation. This method reveals an effective strategy for the synthesis of enantioenriched α-C H aminated derivatives which is hitherto challenging. The choice of the robust chiral indabox ligand was ascertained to be very crucial for the desired enantioselectivity in the contemporary transformation. The reaction mechanism is fully supported by ab initio electronic structure calculations. The reaction is facile, efficient and performs well at room temperature with an enantiomeric excess (ee) up to 93 %.