Abstract
AbstractHydrocarbazolones are a key structural unit in many natural bioactive compounds and are thus a valuable synthetic target. A rhodium‐catalyzed C−H functionalization reaction with acceptor/acceptor diazo compounds was developed for synthesizing 2,3‐fused indole variants. An α,β‐unsaturated enone was utilized as a directing group for site‐selective C−H activation and as an electrophile for the subsequent cyclization. Overall, the developed annulation enabled the rapid assembly of synthetically valuable hydrocarbazolones from readily available indoles. Additionally, computational investigations were conducted to elucidate the reaction pathway and rationalize the experimentally observed site‐selectivity.magnified image
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