Ni-catalyzed C–F activation to construct C–P bond with P–P(O) and P(O)OR mediation

Abstract

Here we developed an efficient Ni-catalyzed C–F bond phosphorylation of aryl fluorides via the crucial intermediates of P–P(O) and P(O)OR. P–P(O) mediated organophosphorus generation is observed for active aryl fluorides, whereas inactive aryl fluorides can also be activated and phosphorylated via a P(O)OR-mediated pathway, which is barely reported yet. Facile scale-up to the gram level and the upgrading of the bioactive molecule make this protocol to have promising applications in synthetic chemistry.