Selective perfluoroalkylation and defluorination functionalization of Indoles

Abstract

The selective activation and functionalization of C-F bonds remain significant challenges in synthetic and medicinal chemistry. Herein, we report a solvent-promoted strategy for selective C-F bond activation, enabling the hydrodefluorination and hydroxydefluorination of indole using heptafluoro-2-iodopropane in the presence of sodium dithionite (Na₂S₂O₄). This method offers efficient access to a wide range of fluorinated indole derivatives under mild reaction conditions, achieving good yields.