Mild and General Method for the α-Arylation of Heteroaromatic Ketones

The development of a general and mild method for Pd-catalyzed alpha-arylation of a variety of ketones bearing multiple heteroatoms is described. The ligand to metal ratio and the position of the heteroatoms with respect to the carbonyl moiety significantly impact the efficiency of these transformations. In addition, these conditions were successfully applied to the alpha-arylation of cyclic imines. A detailed investigation of the scope of this methodology, including the effect of the ligand to metal ratio, is discussed.