A sequential one-pot two-step reaction for efficient synthesis of pyrrolo[2,1-a]isoquinoline and pyrrolo[1,2-a]- quinoline derivatives in good yields has been successfully developed. The reaction included firstly Cu-catalyzed three-component reaction of isoquinoline (quinoline), acetylenedicarboxylate and alkynylbenzene and then Pd-catalyzed intramolecular C(sp)-C(sp^2) coupling reaction of initially formed 1-alkenyl-2-alkynyl- 1,2-dihydroiso- quinoline (1,2-dihydroquinoline).
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