Direct Amination of α-Hydroxy Amides

The TiCl4-mediated reaction for the direct amination of α-hydroxy amide has been developed. This simple, general, additive/base/ligand-free reaction is mediated by economical TiCl4. The reaction runs under mild condition. This highly efficient C-N bond formation protocol is valid for diverse amines, including primary, secondary, heterocyclic and even primary amide and indole.