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Experimental study demonstrates rhodium-catalyzed C2-alkylation of indoles with cyclopropanols, enabling concise synthesis of indole-fused seven-membered heterocycles.
A Rh(III)-catalyzed oxidative C2-alkylation of indoles with cyclopropanols has been successfully developed to generate various β-indolyl ketones with good functional group compatibility under mild reaction conditions. Notably, the newly incorporated carbonyl moiety in the N-carboxamide indole products can serve as a versatile synthetic handle, allowing the straightforward construction of two different classes of indole-fused seven-membered heterocycles via a concise two-step derivatization.
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Liang et al. (2026) studied this question.
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