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Amine Activation: Synthesis of N-(Hetero)arylamides from Isothioureas and Carboxylic Acids

Yan-Ping Zhu, Sergey Sergeyev, Philippe Franck, Romano V. A. Orru and Bert U. W. Maes*

*Organic Synthesis, Department of Chemistry, University of Antwerp, Groenenborgerlaan 171, 2020 Antwerp, Belgium, Email:

Y.-P. Zhu, S. Sergeyev, P. Franck, R. V. A. Orru, B. U. W. Maes, Org. Lett., 2016, 18, 4602-4605.

DOI: 10.1021/acs.orglett.6b02247

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A method for N-(hetero)arylamide synthesis based on rarely explored amine activation, rather than classical acid activation, shows a broad scope including challenging amides. The activated amines are easily prepared using a three-component reaction with commercial reagents.

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Key Words


ID: J54-Y2016