Design and Development of an Organocatalyst for Light Accelerated Amide and Peptide Synthesis

Abstract

The catalytic methods for amide and peptide synthesis have long been recognized as some of the most pressing challenges in industry and academia. Designing more attractive catalysts is crucial to addressing these challenges. Herein, we report a simple organocatalyst, named Cat-Se, for the direct synthesis of amides and peptides. The catalyst can simultaneously avoid many application barriers, thereby providing a good boost to applied research in the field. It can rapidly catalyze various carboxylic acids and amines to form amides in high yields under mild light irradiation conditions without any undesirable operations. The method exhibits high selectivity and maintains stereochemical integrity during peptide synthesis. Significantly, Cat-Se also shows effectiveness in peptide fragment condensation and solid-phase peptide synthesis, making it an attractive method for peptide drug synthesis.

Cat-Se can catalyze amide/peptide synthesis under mild light. It shows high yield, stereoselectivity, and compatibility with SPPS, advancing sustainable catalytic methods for peptide drug synthesis.