On-resin macrocyclization of peptides via intramolecular SnAr reactions

被引：16

作者：

Fotsch, C

Kumaravel, G

Sharma, SK

Wu, AD

Gounarides, JS

Nirmala, NR

Petter, RC

机构：

[1] Novartis Pharmaceut, Dept Transplantat, E Hanover, NJ 07936 USA

[2] Novartis Pharmaceut, Dept Oncol, E Hanover, NJ 07936 USA

[3] Novartis Pharmaceut, Dept Core Technol, E Hanover, NJ 07936 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 15期

关键词：

D O I：

10.1016/S0960-894X(99)00356-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

On-resin macrocyclization via an SNAr reaction is employed in the synthesis of tocinoic acid analogs. Specifically, an N-terminal nitrofluorobenzene is attacked by a nucleophilic C-terminal sidechain. The remaining nitro group can be reduced and acylated. NMR is used to compare the conformation of the new macrocyclic peptides to tocinoic acid. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：2125 / 2130

页数：6

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[21] 1-HYDROXY-7-AZABENZOTRIAZOLE - AN EFFICIENT PEPTIDE COUPLING ADDITIVE [J].