Optically active α-amino acid derivatives were accessed through the direct asymmetric α-amination of α-substituted β-ketoesters 1, catalyzed by chiral CuII–bisoxazoline (BOX) complexes. The reaction proceeds with dibenzyl azodicarboxylate in the presence of only 0.2 mol % of the catalyst to give the desired products 2 in high yield with excellent enantioselectivity (up to 99 % ee).
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