Pd0/PR3-Catalyzed Arylation of Nicotinic and Isonicotinic Acid Derivatives


  • We gratefully acknowledge The Scripps Research Institute, the National Institutes of Health (NIGMS, 1 R01 GM084019-02), Amgen, and Eli Lilly for financial support. We thank the A. P. Sloan Foundation for a fellowship (J.-Q.Y.), and the Bristol Myers Squibb for a graduate fellowship (M.W.).


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Good for your health: Intermolecular C[BOND]H functionalization of pyridine rings at the 3- and 4-positions is described using a Pd0/PR3/ArBr catalytic system. This reaction provides a powerful method for the preparation of structurally diverse nicotinic and isonicotinic acids that are of great importance in drug discovery.