☆ 3.8 Article

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

JOURNAL OF COMBINATORIAL CHEMISTRY (2009)

期刊

JOURNAL OF COMBINATORIAL CHEMISTRY

卷 11, 期 6, 页码 1066-1072

出版社

AMER CHEMICAL SOC

DOI: 10.1021/cc900100z

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Chemistry, Applied Chemistry, Medicinal Chemistry, Multidisciplinary

资金

National Science Foundation [0455072]
State of Florida
Executive Officer of the Governor's Office of Tourism
Trade and Economic Development [IP41GM079590, 1P41GM081261, U54HG03916-MLSCN]
Division Of Chemistry
Direct For Mathematical & Physical Scien [0455072] Funding Source: National Science Foundation

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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 oil 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.

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