Pyridine Synthesis via [3 + 2 + 1] Oxidative Cyclization of Enamines, Ethyl Tertiary Amines, and Alcohols: Copper-Catalyzed Cascade Multicomponent Poly C(sp ³ )–H Functionalization

A copper-catalyzed [3 + 2 + 1] oxidative cyclization to access functionalized pyridines was descripted. Employing ethyl tertiary amine as a C2 source, alcohol as a C1 source, and easily handled enamines, one new C–N bond and two new C–C bonds are sequentially constructed by the effective functionalization of multiple C(sp 3 )–H bonds. Besides the readily available raw materials, mild reaction conditions, broad substrate scope, and effective bond-forming strategy, the present approach offers a viable strategy for preparing functionalized pyridines in future organic synthesis.