Ru(II)-Catalyzed annulation of benzamidines and alkynes by C–H/N–H activation: a facile synthesis of 1-aminoisoquinolines

An inexpensive Ru(II) complex catalyzes the oxidative annulation reaction of disubstituted alkynes with benzamidines to provide highly valuable 1-aminoisoquinolines in high yields. The reaction also features excellent regioselectivity with some unsymmetrical alkynes.