Max-Planck-Institut für Kohlenforschung, Kaiser-Wilhelm-Platz 1, 45470 Mülheim an der Ruhr (Germany).
Angew Chem Int Ed Engl. 2014 May 19;53(21):5462-6. doi: 10.1002/anie.201402229. Epub 2014 Apr 16.
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.
本文提出了一种酰胺α-芳基化的全新方法,通过亲电酰胺活化,芳基可以区域选择性地α-引入酰胺中,即使存在酯和烷基酮也是如此。机理研究揭示了关键反应中间体,并强调了该转化中非常微妙的碱效应。