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. 2022 Jun 30;58(53):7435-7438.
doi: 10.1039/d2cc01551j.

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

Alexander Burtea  1 , Jacob DeForest  1 , Neil Baldwin  2 , Carolyn Leverett  2 , Gary M Gallego  1
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A convenient and versatile SNAr-decarboxylation protocol for the construction of C(sp2)-C(sp3) bonds

Alexander Burtea et al. Chem Commun (Camb). .

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.

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