Copper-catalyzed synthesis of α-ketoamides using water and dioxygen as the oxygen source.

The reaction employing HO and O as the co-oxygen source in the catalytic synthesis of α-ketoamides is described. This copper-catalyzed reaction is carried out in a tandem manner constituted by the hydroamination of alkyne, hydration of vinyl-Cu complex and subsequent oxidation. Isotope labeling and radical capture experiments reveal that the oxygen atom of α-ketone at α-ketoamides derives from O and the oxygen atom of amide group originates from HO.