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Potassium tert-Butoxide Facilitated Amination of Carboxylic Acids with N,N-Dimethylformamide

Yuanjing Huang, Jing Zhang*

*The Institute for Advanced Studies (IAS), Wuhan University, 299 Bayi Rd, Wuhan 430072, P. R. of China, Email: jzhangwhuwhu.edu.cn

Y. Huang, J. Zhang, Synthesis, 2022, 54, 3595-3604.

DOI: 10.1055/a-1817-1965


Abstract

The combination of trimethylacetic anhydride and catalytic amounts of potassium tert-butoxide mediates an amination of carboxylic acids with DMF as a dimethylamine reagent to provide N,N-dimethylamides. The applicability of this protocol is demonstrated by late-stage dimethylamidations of complex drug molecules.

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Key Words

amidation, N,N-dimethylformamide, carboxylic acids, potassium tert-butoxide


ID: J66-Y2022