Base-Promoted [4+3] Annulation Reaction of Indole-2-carboxamides with β-CF3-1,3-Enynes: Access to Fluorine-Containing Indole-1,2-Fused 1,4-Diazepinones

Abstract

An efficient base-promoted approach for the synthesis of fluorine-containing indole-1,2-fused 1,4-diazepinones via [4+3] annulation of indoles with β-CF3-1,3-enynes is presented. This strategy delivers the target products in good to excellent yields under the mild reaction conditions, showcasing high step economy and broad substrate scope. This reaction could be scalable to gram and amenable to diverse functionalization, underscoring its potential utility in pharmaceutical development and materials science.