Organocatalyst Enabled Light Accelerated Amide and Peptide Synthesis

Abstract Catalytic methods for amide and peptide synthesis have long been recognized as one of the most pressing challenges in industry and academia, requiring novel catalysts to meet this requirement. Herein, we report an organocatalyst, named Cat-Se, for direct amide and peptide synthesis. Cat-Se, which has a simple and exquisite chemical structure, can be conveniently synthesized and catalyzes the condensation of various carboxylic acids and amines to the corresponding amides in excellent yields within 30-40 minutes under very mild light irradiation conditions without any undesirable operations, such as heating, dehydration, or gas protection. The method exhibits high efficiency, selectivity, and functional group tolerance without loss of stereochemical integrity in peptide synthesis. Significantly, Cat-Se shows power in peptide fragment condensation and solid-phase peptide synthesis on resin, making it an attractive alternative for peptide drug synthesis.