Catalytic amidation of unactivated ester derivatives mediated by trifluoroethanol

被引：55

作者：

Caldwell, Nicola ^{[1
]}

Jamieson, Craig ^{[1
]}

Simpson, Iain ^{[2
]}

Watson, Allan J. B. ^{[1
]}

机构：

[1] Univ Strathclyde, Dept Pure & Appl Chem, Glasgow G1 1XL, Lanark, Scotland

[2] AstraZeneca, Oncol Innovat Med, Cambridge CB4 0WG, England

来源：

CHEMICAL COMMUNICATIONS | 2015年 / 51卷 / 46期

关键词：

DIRECT AMIDE FORMATION; CARBOXYLIC-ACIDS; MEDICINAL CHEMISTS; MILD; ALCOHOLS; AMINES;

D O I：

10.1039/c5cc02895g

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A catalytic amidation method has been developed, employing 2,2,2-trifluoroethanol to facilitate condensation of unactivated esters and amines, enabling the synthesis of a range of amide products in good to excellent yields. Mechanistic studies indicate the reaction proceeds through a trifluoroethanol-derived active ester intermediate.

引用

页码：9495 / 9498

页数：4

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