Palladium-Catalyzed Cascade Synthesis of Novel Quinolone- Bis(indolyl)methane Hybrids as Promising α-Glucosidase Inhibitors

Abstract An unexpected cascade reaction is developed for the construction of functionalized 3-bis(indol-3-yl)methylquinoline-2(1H)-ones. Three C–C bonds and one ring are created in one pot triggered by Pd-catalyzed C-3 alkenylation of indole with 2-acyl-N-acrylaniline derivatives. A series of complex and specific quinoline-2(1H)-ones were produced, most of them showed significant α-glucosidase inhibitory activities.