A General Method for Aminoquinoline-Directed, Copper-Catalyzed sp2 C-H Bond Amination

An operationally simple and general method for copper-catalyzed, aminoquinoline-assisted amination of beta-C(sp(2))-H bonds of benzoic acid derivatives is reported. The reaction employs Cu(OAc)(2) or (CuOH)(2)CO3 catalysts, an amine coupling partner, and oxygen from air as a terminal oxidant. Exceptionally high generality with respect to amine coupling partners is observed. Specifically, primary and secondary aliphatic and aromatic amines, heterocycles, such as indoles, pyrazole, and carbazole, sulfonamides, as well as electron-deficient aromatic and heteroaromatic amines are competent coupling components.