Synthesis of Indolizines via Tf2O-Mediated Cascade Reaction of Pyridyl-enaminones with Thiophenols/Thioalcohols

Org Lett. 2023 Feb 24;25(7):1192-1197. doi: 10.1021/acs.orglett.3c00177. Epub 2023 Feb 13.

Abstract

A cost-effective, highly regioselective and metal-free version for the synthesis of indolizine derivatives by means of Tf2O-mediated cascade reaction of pyridyl-enaminones and thiophenols/thioalcohols under mild reaction conditions has been reported. Diverse electron-rich indolizine derivatives could be obtained in up to 94% yield via the selective 1,4-addition of vinyl iminium triflate tandem cyclization/aromatization, which allowed the simultaneous construction of C-N and C-S/and one example of C-Se bonds.