Multiple Oxidative Dehydrogenative Functionalization of Arylacetaldehydes Using Molecular Oxygen as Oxidant Leading to 2-Oxo-acetamidines

A novel copper-catalyzed, multiple oxidative dehydrogenative functionalization of arylacetaldehydes leading to 2-oxo-acetamidine compounds has been developed. This transformation is highly efficient with dissociation of six hydrogens including two sp3 C?H and one sp2 C?H bond activations. This method not only provides an efficient approach to 2-oxo-acetamidine compounds, but also offers a valuable mechanistic insight into this novel copper catalysis.