Ligand-free CuI-catalyzed selective C-N coupling of aliphatic amino group of α-amino acid amides with ortho-dihaloarenes

Selective C-N coupling of aliphatic amino group of α-amino acid amides is a direct and valuable method, but it still remains unresolved. Here we disclose a simple and cheap ligand-free CuI-catalyzed selective synthesis of chiral N-(2-halo(hetero)aryl) amino acid amides without obvious racemization.