Divergent C–H Functionalizations Directed by Sulfonamide Pharmacophores: Late-Stage Diversification as a Tool for Drug Discovery

Hui-Xiong Dai, Antonia F. Stepan, Mark S. Plummer, Yang-Hui Zhang, and Jin-Quan Yu

J. Am. Chem. Soc.,
2011, 133, (18), 7222-7228; 10.1021/ja201708f


Modern drug discovery is contingent on identifying lead compounds and rapidly synthesizing analogues. The use of a common pharmacophore to direct multiple and divergent C–H functionalizations of lead compounds is a particularly attractive approach. The Yu group, in collaboration with Pfizer, describe an effective method to acheive this using C–H Functionalization.

C–H Functionalization is an attractive method to achieve such late-stage functionalization of a scaffold of interest as it is not relient on the incorporation of functionality or reactive centers, instead capable of employing the 'inert' skeleton of the molecule.

As the toolbox of selective catalysts and transformations expands within the CCHF a greater scope of selective late-stage C–H functionalization will be possible.

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