Molecular Iodine‐Catalysed Reductive Alkylation of Indoles: Late‐Stage Diversification for Bioactive Molecules

Abstract

AbstractHerein, we report a molecular iodine‐catalysed reductive alkylation of indoles with carbonyl compounds using Et3SiH for the efficient synthesis of C3‐alkylated indoles. This metal‐free and environmental‐friendly process exhibits excellent functional group tolerance, mild conditions, and wide substrate scope. Notably, the synthetic usefulness of this strategy to pharmacochemistry was highlighted by the late‐stage modification of drug‐like molecules.