环四肽在药物研发中具有重要的潜在应用价值,然而目前尚缺乏高效率合成环四肽的方法.我们发展了以N端为半胱氨酸的四肽酰肼为原料的分子内环化方法,合成了全L型氨基酸组成的环四肽.该方法通过形成13元环的内硫酯中间体,再经过S-to-N酰基迁移形成酰胺键,最后通过脱硫反应,得到目标环四肽分子. Cyclic tetrapeptides have important potential applications in the drug development, however, there is a lack of efficient synthesis of cyclic tetrapeptides.We have developed intramolecular cyclization starting from tetrapeptide hydrazide with N-terminal cysteine Method, the synthesis of a full-L amino acid composition of cyclic tetrapeptide by the formation of thirteen ring internal thioester intermediates, and then S-to-N acyl to form amide bond transfer, and finally by desulfurization reaction, the target ring four Peptide molecule.