Chemoselective intermolecular α-arylation of amides

Angew Chem Int Ed Engl. 2014 May 19;53(21):5462-6. doi: 10.1002/anie.201402229. Epub 2014 Apr 16.

Abstract

A new approach for the fully chemoselective α-arylation of amides is presented. By means of electrophilic amide activation, aryl groups can be regioselectively introduced α- to amides, even in the presence of esters and alkyl ketones. Mechanistic studies reveal key reaction intermediates and emphasize a remarkably subtle base effect in this transformation.

Keywords: amides; arylation; chemoselectivity; keteniminium ions; sulfoxides.