A simple and efficient copper-catalyzed three-component reaction to synthesize ()-1,2-dihydro-2-iminoquinolines.

A operationally simple synthesis of ()-1,2-dihydro-2-iminoquinolines that proceeds under mild conditions is achieved by copper-catalyzed reaction of 1-(2-aminophenyl)ethan-1-ones, sulfonyl azides and terminal ynones. In particular, the reaction goes through a base-free CuAAC/ring-opening process to obtain the -configured products due to hydrogen bonding.