Nickel-Catalyzed Reductive Arylation of gem-Bromofluorocyclopropanes To Construct Monofluorinated Cyclopropane Derivatives

Abstract

A nickel-catalyzed reductive cross-coupling of gem-bromofluorocyclopropanes with aryl bromides for the synthesis of monofluorinated cyclopropane derivatives is reported. Different from the cleavage route of the cyclopropane ring reported by previous works, this catalytic system shows excellent regioselectivity control of cyclic selectivity, giving monofluorinated cyclopropane derivatives as the major product. This transformation demonstrates mild conditions, high efficiency, a broad substrate scope, and good functional group compatibility, providing a facile method for the synthesis of diversified monofluorinated cyclopropane-containing drugs and bioactive molecules.