Copper-catalyzed radical cascade cyclization for synthesis of CF3-containing tetracyclic benzimidazo[2,1-a]iso-quinolin-6(5H)-ones.

Here, a general copper-catalyzed radical cascade carbocyclization reaction with 2-arylbenzoimidazoles and a Togni reagent was realized. Structurally diverse CF3-containing tetracyclic core benzimidazo[2,1-a]isoquinoline-6(5H)-ones were obtained in moderate to good yields. The wide substrate scope, good functional group tolerance, and ease of scale-up of this method are expected to promote its potential applications in pharmacy and biotechnology.