Synthesis of di/trifluoromethyl cyclopropane-dicarbonitriles via [2+1] annulation of fluoro-based diazoethanes with (alkylidene)malononitriles

Abstract

Herein, we describe a [2+1] annulation reaction of di/trifluorodiazoethane with (alkylidene)malononitriles. This protocol offers a streamlined synthesis of a wide range of stereospecific and densely functionalized difluoromethyl and trifluoromethyl cyclopropane-1,1-dicarbonitriles. Further functional group interconversions or skeletal elaborations afford structurally distinct cyclopropyl variants.