A convenient and versatile S N Ar-decarboxylation protocol for the construction of C(sp 2 )-C(sp 3 ) bonds.

Increasing saturation (Fsp 3 ) 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(sp 2 )-C(sp 3 ) bonds. The method is tolerant of a variety of biologically privileged moieties and has been demonstrated in a library format.