Solid phase synthesis of 'head-to-tail' cyclic peptides using a sulfonamide 'safety-catch' linker: the cleavage by cyclization approach

被引：71

作者：

Yang, LH ^{[1
]}

Morriello, G ^{[1
]}

机构：

[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA

来源：

TETRAHEDRON LETTERS | 1999年 / 40卷 / 47期

关键词：

cyclization; peptides; polypeptides; solid-phase synthesis; combinatorial chemistry;

D O I：

10.1016/S0040-4039(99)01701-3

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A new approach to the synthesis of cyclic peptides using Kenner's 'safety-catch' sulfonamide linker is described. After the linear peptide is assembled by Fmoc peptide synthesis, trityl is adopted as a temporary protecting group for the N-terminus amine while activating the acyl sulfonamide linker. Head-to-tail cyclization-cleavage of the amine to the acyl sulfonamide ensured final product purity. (C) 1999 Elsevier Science Ltd. All rights reserved.

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页码：8197 / 8200

页数：4

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