Application of epimerisation-free amide coupling conditions to the synthesis of matrix metalloprotease inhibitor intermediates.

被引：10

作者：

Fray, MJ ^{[1
]}

Ellis, D ^{[1
]}

机构：

[1] Pfizer Cent Res, Dept Discovery Chem, Sandwich CT13 9NJ, Kent, England

来源：

TETRAHEDRON | 1998年 / 54卷 / 45期

关键词：

D O I：

10.1016/S0040-4020(98)00836-9

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Coupling of the N-acyl tert-leucine derivative 2 with a variety of amines 3a-g gave amides 4a-g in good to excellent yields (75-95%) with minimal epimerisation (less than or equal to 3%) at the tert-leucine stereogenic centre. Limitations of the method are discussed. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：13825 / 13832

页数：8

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