Tf₂O-activated modular assembly of tetrasubstituted alkenes

Abstract

Tetrasubstituted alkenes, particularly those bearing C(sp²)-S and C(sp²)-N bonds, represent pivotal structural motifs in bioactive molecules, yet their synthesis remains a significant challenge. This study introduces a novel, efficient, multicomponent strategy for constructing these motifs with high stereoselectivity and broad substrate compatibility through Tf₂O-mediated carbonyl compound activation. Mechanistic investigations reveal a stepwise process involving formation of enol triflate intermediates and subsequent nucleophilic addition.