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Metal-Free Amidation of Acids with Formamides and T3P®

Linda Bannwart, Stefan Abele, Simone Tortoioli*

*Chemistry Process R&D, Actelion Pharmaceuticals Ltd., Gewerbestrasse 16, 4123 Allschwil, Switzerland, Email: simone.tortoioliactelion.com

L. Bannwart, S. Abele, S. Tortoioli, Synthesis, 2016, 48, 2069-2078.

DOI: 10.1055/s-0035-1561427


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Abstract

A simple and metal-free method for the direct formation of dialkylamides from carboxylic acids employs N,N-dialkylformamides as amine source. The one-pot reaction is promoted by propylphosphonic anhydride (T3P®) in the presence of 0.5 equivalents of HCl.

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Key Words

formamides, propylphosphonic anhydride, amidation, carboxylic acids, metal-free


ID: J66-Y2016