2-Perfluoroalkylated indoles were efficiently synthesized via a one-pot cascade Michael-type addition/palladium-catalyzed intramolecular cross-dehydrogenative coupling (CDC) process, using molecular oxygen as the sole oxidant at 100 °C in DMSO. This process allows atom economical assembly of indole rings from inexpensive and readily available anilines and methyl perfluoroalk-2-ynoates and tolerates a broad range of functional groups.

A facile multi‐component process for the synthesis of perfluoroalkylated quinolizine derivatives was achieved using various arylidenemalononitriles, pyridine, and methyl perfluoroalk‐2‐ynoates as starting materials. Moderate yields were obtained under mild condition. The structures of perfluoroalkylated quinolizine derivatives were characterized by means of 1H NMR, 13C NMR, 19F NMR, IR, LRMS and HRMS. Furthermore, the reaction mechanism was proposed.

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This protocol utilizes molecular oxygen as terminal oxidant and shows high regioselectively with respect to the formation of 2‐trifluoroalkyl indoles.