Rhodium(III)-Catalyzed Direct C–H Alkylation of Indoles with Cyclopropanols and Its Application in the Divergent Synthesis of Indole-Fused Seven-Membered Heterocycles

Abstract

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.