Copper-catalyzed, hypervalent iodine mediated CC bond activation of enaminones for the synthesis of α-keto amides

Abstract

An unprecedented CC bond cleavage of enaminones has been realized by means of copper catalysis in the presence of hypervalent iodine (PhI(OAc)₂). The cascade transformation based on this bond cleavage leads to the synthesis of various α-keto amides. Isotope labeling experiments suggest that water has acted as a source of oxygen atoms during the generation of the new carbonyl group.