Convenient N-acetylation of amines in N,N-dimethylacetamide with N,N-carbonyldiimidazole

被引:27
|
作者
Chikkulapalli, Anil [1 ,2 ]
Aavula, Sanjeev Kumar [1 ]
Mona, Rifahath N. P. [1 ]
Karthikeyan, C. [1 ]
Kumar, Vinodh C. H. [1 ]
Sulur, Manjunatha G. [1 ]
Sumathi, Shanmugam [2 ]
机构
[1] AstraZeneca India Pvt Ltd, Pharmaceut Dev, Bangalore 560024, Karnataka, India
[2] VIT Univ, Sch Adv Sci, Vellore 632014, Tamil Nadu, India
关键词
Acetylation; Amines; Carbonyldiimidazole; N; N-Dimethylacetamide; Imidazole; CARBOXYLIC-ACIDS; ACYLATION; ALCOHOLS; EFFICIENT; AMIDE; ANHYDRIDES; PHENOLS; ESTERIFICATION; CATALYST; REAGENT;
D O I
10.1016/j.tetlet.2015.04.077
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Dimethylacetamide (DMAc) acts as an efficient source of acetyl and dimethylamine gas in the presence of N,N-carbonyldiimidazole (CDI). Addition of amines to the reaction mixture delivers the corresponding amides in good to excellent yields. The acetylation of amines reported herein, which relies on the in situ generation of N-acetylimidazole on warming of DMAc with CDT at 120-125 degrees C, serves as a convenient alternative to other acetylation methods. (C) 2015 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3799 / 3803
页数:5
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