An efficient synthesis of 6-arylbenzo[4,5]imidazo[2,1-a]isoquinolines via sequential α-arylation of carbonyl and deacylation catalyzed by CuI.

Dibenzoyl methane was found to undergo α-arylation of carbonyl and deacylation reaction with 2-(2-bromophenyl)-1H-benzo[d]imidazoles catalyzed by CuI in the presence of Cs2CO3, and provided an efficient synthesis of 6-arylbenzo[4,5]imidazo[2,1-a]isoquinolines via subsequent intra-molecular nucleophilic addition and dehydration.