Construction of the tetrahydroquinoline spiro skeleton via cascade [1,5]-hydride transfer-involved C(sp3)–H functionalization “on water”

Abstract

The pharmaceutically important tetrahydroquinoline spiro compounds were efficiently constructed via cascade S_NAr/Knoevenagel condensation/[1,5]-hydride transfer/cyclization on water, featuring high atom-economy and step-economy. This water-based redox-neutral C(sp³)–H functionalization rendered a 4-step cascade reaction successful without resorting to any catalysts.