Functionalization of Quinolines through Copper‐Catalyzed Regioselective Halogenation Reaction

Abstract A copper‐catalyzed chelation‐controlled remote C–H halogenation of quinolines is developed. The reaction is scalable and proceeded with excellent C5‐regioselectivity offering halogen‐substituted 8‐aminoquinolines in very high yields (up to 97 %). The products were further utilized for various cross‐coupling reactions en route to highly C5‐functinonalized quinolines. As an application, synthesis of a bioactive compound having tumor‐suppressor activity was accomplished.