A convenient and versatile SNAr-decarboxylation protocol for the construction of C(sp2)–C(sp3) bonds

Abstract

Increasing saturation (Fsp³) remains a central strategy in the optimization of properties of molecules during drug discovery. Here, we describe a versatile and operationally simple one-pot procedure for accomplishing this goal via a nucleophilic aromatic substitution-decarboxylation sequence to construct C(sp²)–C(sp³) bonds. The method is tolerant of a variety of biologically privileged moieties and has been demonstrated in a library format.