Li Yiping, Li Jingyue, Shen Zhouming, Kuang Haoyu, Zuo Quan, Bao Guangjun, Ni Jingman, Sun Wangsheng, Wang Rui
Key Laboratory of Preclinical Study for New Drugs of Gansu Province, School of Basic Medical Sciences & Research Unit of Peptide Science, Chinese Academy of Medical Sciences, 2019RU066, Lanzhou University, Lanzhou 730000, Gansu, P. R. China.
State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, P. R. China.
ACS Cent Sci. 2025 Jun 30;11(7):1240-1249. doi: 10.1021/acscentsci.5c00487. eCollection 2025 Jul 23.
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.
酰胺和肽合成的催化方法长期以来一直被认为是工业界和学术界面临的一些最紧迫的挑战。设计更具吸引力的催化剂对于应对这些挑战至关重要。在此，我们报道了一种名为Cat-Se的简单有机催化剂，用于直接合成酰胺和肽。该催化剂可以同时避免许多应用障碍，从而有力地推动了该领域的应用研究。它可以在温和的光照条件下快速催化各种羧酸和胺以高收率形成酰胺，无需任何繁琐操作。该方法具有高选择性，并且在肽合成过程中保持立体化学完整性。值得注意的是，Cat-Se在肽片段缩合和固相肽合成中也显示出有效性，使其成为一种有吸引力的肽药物合成方法。
