Copper-Catalyzed Oxidative C–H Annulation of Quinolines with Dichloroethane toward Benzoquinoliziniums Using an In Situ Activation Strategy

Described herein is a copper-catalyzed oxidative C–H annulation of quinolines with 1,2-chloroethane (DCE), providing a concise synthetic approach to benzoquinoliziniums. In this protocol, DCE not only serves as a solvent and an in situ activation agent of quinoline C2–H but also works as vinyl equivalents to constitute the six-membered azonia ring. Furthermore, the resultant benzoquinolizinium library exhibits good properties of binding to DNA and low cytotoxicity.