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

The reaction employing H(2)O and O(2) 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(2) and the oxygen atom of amide group originates from H(2)O.