Catalytic highly enantioselective direct amination of 1,3-diketones

The direct asymmetric amination of 1,3-diketones by azodicarboxylates catalyzed by chiral copper(II) bisoxazolines is presented. Screening of chiral bisoxazoline ligands, Lewis acids, solvents, and other reaction parameters led to an enantioselective direct amination in the 2-position of 1,3-diketones and the optically active functionalized molecules were obtained in high yields and enantioselectivities.