Highly diastereoselective peptide chain extensions of unprotected amino acids with N-(Z-α-aminoacyl)benzotriazoles

被引：71

作者：

Katritzky, AR ^{[1
]}

Suzuki, K ^{[1
]}

Singh, SK ^{[1
]}

机构：

[1] Univ Florida, Dept Chem, Ctr Hetetocycl Cmpds, Gainesville, FL 32611 USA

来源：

SYNTHESIS-STUTTGART | 2004年 / 16期

关键词：

benzotriazole methodology; N-(Z-alpha-aminoacyl)benzotriazole; peptide coupling; peptides;

D O I：

10.1055/s-2004-831255

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Coupling an unprotected amino acid or dipeptide in partially aqueous solution with a readily available N-(Z-alpha-aminoacyl)benzotriazole or N-(Z-alpha-aminopetidoyl)benzotriazole affords N-terminal-protected di-, tri-, and tetrapeptides in yields of 85-98% (average 95% for 2a-i, 93% for 4a-f and 4a', 86% for 5a-b) with minimal epimerization.

引用

页码：2645 / 2652

页数：8

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