Nucleopalladation strategy towards regioselective N-alkylation of indoles with unactivated olefins

Abstract

A regioselective intermolecular nucleopalladation of indolines with unactivated olefins followed by oxidation is developed to access valuable N-alkyl indoles in high yields. This one-pot protocol features operational simplicity, scalability, and offers a strategic means to circumvent the intrinsic carbon-centered reactivity of indoles. Additionally, downstream product diversification was demonstrated through the functionalization of C(sp²)–H and C(sp³)–H bonds.