The development of modern and emerging catalysis protocols for aromatic C-C, C-N, C-O, C-S, and C-F bond formation to prepare medicinally active biaryls, amines, ethers, sulfides, sulfones, and aryl fluorides has had a tremendous impact in the speed and efficiency by which medicinal chemists develop and identify optimal molecules, both preclinical candidates as well as proof-of-concept probe molecules.  In addition, for preclinical candidates, modern catalysis C-X cross-coupling has readily extended its reach to process chemistry, impacting the efficiency of drug candidate GMP delivery.  This presentation will focus on protease and GPCR target classes wherein an aspect of the structure-activity-relationship (SAR) proved formidable in terms of disposition (e.g. CNS), potency, or selectivity and how catalysis C-X cross-coupling protocols played a role in leading to the identification of molecules which addressed a key issue or led to an unexpected benefit in the target profile.

Catalysis driven medicinal chemistry and challenges in protease and allosteric GPCR space

248th National Meeting (2014)

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