Development of a Sustainable Catalytic Ester Amidation Process

被引：36

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, WestCHEM, Glasgow G1 1XL, Lanark, Scotland

[2] AstraZeneca, Oncol Innovat Med Unit, Macclesfield SK10 4TG, Cheshire, England

来源：

ACS SUSTAINABLE CHEMISTRY & ENGINEERING | 2013年 / 1卷 / 10期

基金：

英国工程与自然科学研究理事会;

关键词：

Amidation; Green solvents; Replacement bases; Reaction screening; Design of Experiments; DIRECT AMIDE FORMATION; CARBOXYLIC-ACIDS; ALTERNATIVE SOLVENTS; MEDICINAL CHEMISTS; REPLACEMENT; SELECTION; AMINES; DICHLOROMETHANE; OPTIMIZATION; PERSPECTIVE;

D O I：

10.1021/sc400204g

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

We describe the development of a sustainable ester amidation process. Base and solvent screening, combined with the application of Design of Experiments methodology was employed to identify an optimized set of reaction conditions using a sustainable protocol. Utilizing these optimized conditions, treatment of a range of ester derivatives with amino alcohols in the presence of a catalytic quantity of potassium phosphate deploying iso-propanol as solvent results in the highly efficient generation of a range of amido-alcohol derivatives in good to excellent yield, accompanied with excellent reaction mass efficiency (RME).

引用

页码：1339 / 1344

页数：6

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