使用1-乙基-3-(3-二甲基氨基丙基)碳二亚胺（EDC）、4-二甲氨基吡啶（DMAP）和催化量的1-羟基苯并三唑（HOBt）作为偶联试剂，合成缺电子胺和功能化羧酸的酰胺衍生物。
Synthesis of amide derivatives for electron deficient amines and functionalized carboxylic acids using EDC and DMAP and a catalytic amount of HOBt as the coupling reagents.
作者信息
Ghosh Arun K, Shahabi Dana
机构信息
Department of Chemistry, Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, Indiana 47907, United States.
出版信息
Tetrahedron Lett. 2021 Jan 19;63. doi: 10.1016/j.tetlet.2020.152719. Epub 2020 Dec 25.
Abstract
A convenient protocol for amide bond formation for electron deficient amines and carboxylic acids is described. Amide coupling of aniline derivatives has been investigated with a number of reagents under a variety of reaction conditions. The use of 1 equivalent of EDC and 1 equivalent of DMAP, catalytic amount of HOBt and DIPEA provided the best results. This method is amenable to the synthesis of a range of functionalized amide derivatives with electron deficient and unreactive amines.
摘要
本文描述了一种用于缺电子胺与羧酸形成酰胺键的简便方法。在多种反应条件下，已用多种试剂研究了苯胺衍生物的酰胺偶联反应。使用1当量的EDC和1当量的DMAP、催化量的HOBt和DIPEA可得到最佳结果。该方法适用于合成一系列含缺电子和无反应性胺的功能化酰胺衍生物。
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