Cu-catalyzed alkylarylation of alkenes via N-directed remote C(sp3)–H functionalization

Abstract

Herein, we report a copper-catalyzed alkylarylation reaction of alkenes using N-fluoroamides and arylboronic acids. The reaction proceeds primarily through nitrogen-centered radical generation, 1,5-hydrogen atom transfer, and benzyl radical addition to provide the target products. This protocol is distinguished by its exquisite site-selectivity, broad substrate scope, and comprehensive utilization of late-stage modification of estrone derivatives. Moreover, this approach offers new insights into synthesizing bioactive molecules with 1,1-diaryl motifs.