Chemoenzymatic synthesis of ketomethylene tripeptide isosteres

被引：4

作者：

Tao, JH ^{[1
]}

Hu, SH ^{[1
]}

Tian, QP ^{[1
]}

Nayyar, N ^{[1
]}

Babu, S ^{[1
]}

机构：

[1] PfizerGlobal R&D, Chem Res & Dev, San Diego, CA 92121 USA

来源：

TETRAHEDRON-ASYMMETRY | 2005年 / 16卷 / 03期

关键词：

D O I：

10.1016/j.tetasy.2004.11.092

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

A chemoenzymatic method is described for the synthesis of a desired ketomethylene tripeptide isostere. The key step is an enzymatic hydrolysis, which removes the C-terminal ester-protecting group under mild conditions without epimerizing the existing stereogenic center and produces the desired stereoisomer in high enantiomeric excess (98% de, 97% ee). The method is short with overall 15-20% yields after seven synthetic steps from readily available starting materials being obtained. (C) 2005 Published by Elsevier Ltd.

引用

页码：699 / 703

页数：5

共 18 条

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