Chemoselective defluorinative amination of (trifluoromethyl)alkenes with amidines: synthesis of 6-fluoro-1,4-dihydropyrimidines

Abstract

The chemoselective defluorinative amination of (trifluoromethyl)alkenes with amidines is reported. This transition-metal-free method is operationally simple and gram-scalable, tolerates diverse useful functional groups, and gives a variety of synthetically valuable 6-fluoro-1,4-dihydropyrimidines in high yields under mild conditions.