Copper-Catalyzed β-Functionalization of Amino Acid Schiff Bases

We have developed a catalytic β-C-H amination of amino acid derivatives using amino acid Schiff bases, which are traditionally employed only in α-functionalization reactions. The present transformation expands the synthetic utility of these widely available building blocks by enabling intermolecular β-C-H amination. Detailed mechanistic studies revealed that the copper catalyst operates via a dual catalytic mode that is essential for the success of the reaction.