C–H Monoarylation of Naphthylpyrimidines with Aryl Chlorides Catalyzed by a Water-Soluble Ruthenium Complex

Selective monoarylation of naphthylpyrimidines with a variety of aryl chlorides through C–H bond activation in water was achieved by using a water-soluble [RuCl 2 -(η 6 -PhOCH 2 CH 2 OH)] 2 /phosphine catalytic system. The monoarylation occurred at the C-2 carbon of the naphthalene moiety, and selectively polysubstituted naphthylpyrimidines were obtained by a one-pot reaction involving a subsequent hetarylation with 2-pyridyl chlorides.