Copper-Catalyzed Cascade Synthesis of Alkyl 6-Aminobenzimidazo[2,1-a]isoquinoline-5-carboxylates

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A convenient and efficient copper-catalyzed cascade method has been developed for synthesis of benzimidazoisoquinoline derivatives via reactions of readily available substituted 2-(2-halophenyl)benzoimidazoles with alkyl cyanoacetates under mild condition, and the corresponding alkyl 6-aminobenzimidazo[2,1-a]isoquinoline-5-carboxylates were obtained in good to excellent yields. The novel method provides diverse and useful poly N-heterocyclic compounds for combinatorial chemistry and medicinal chemistry.