Synthesis of Cyclic Peptides through Direct Aminolysis of Peptide Thioesters Catalyzed by Imidazole in Aqueous Organic Solutions

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• 作者：Yangmei Li ; Austin Yongye ; Marc Giulianotti ; Karina Martinez-Mayorga ; Yongping Yu ; Richard A. Houghten
• 刊名：Journal of Combinatorial Chemistry
• 出版年：2009
• 出版时间：November 9, 2009
• 年：2009
• 卷：11
• 期：6
• 页码：1066-1072
• 全文大小：221K
• 年卷期：v.11,no.6(November 9, 2009)
• ISSN：1520-4774

文摘

A promising method for the synthesis of cyclic peptides through the direct aminolysis of peptide thioesters is presented. The cyclization step was carried out in a mixture of acetonitrile and 1.5 M aqueous imidazole solution with no observable oligomers. Studies on the N- and C-terminal residues show that the choice of C-terminal residue has a more significant effect on the success rate of cyclization than the choice at the N-terminal residue.