A novel one-step synthesis of imidazo[5,1-a]isoquinolines via a tandem Pd-catalyzed alkylation-direct arylation sequence.

A palladium-catalyzed/norbornene-mediated one-step synthesis of highly functionalized imidazoles via a sequential alkyl-aryl and aryl-heteroaryl bond formation is devised. This method provides an efficient route to a wide variety of substituted imidazo[5,1-a]isoquinolines from readily accessible N-bromoalkyl imidazoles and aryl iodides.