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In this new procedure, amide-containing indolo[2,1- a ]isoquinoline scaffolds were prepared by palladium-catalyzed carbonylative cyclization of alkene-tethered indoles with nitroarenes. By using Mo(CO) 6 as the CO source and reductant and nitroarenes as the nitrogen source, this reaction produced various amide-containing indolo[2,1- a ]isoquinoline derivatives in good yields in general. Furthermore, the late-stage modifications of bioactive molecules using this protocol were demonstrated as well.