LIGAND-ENABLED SCALABLE C-H HYDROXYLATION OF BENZOIC AND PHENYLACETIC ACIDS AT ROOM TEMPERATURE

Abstract

The application discloses industry scalable methods of using bifunctional bidentate pyridone-carboxylic acid ligands, such as 2-methyl-2-(6-oxo-1,6-dihydropyridin-2-yl)propanoic acid, that enable room-temperature Pd-catalyzed C—H hydroxylation of a broad range of benzoic and phenylacetic acids with an industry-compatible oxidant, aqueous hydrogen peroxide, at room temperature. Further disclosed are methods of derivatization of the resulting hydroxylation products, synthesis of polyfluorinated natural products coumestan or pterocarpene from phenol building blocks, and hydroxylation of ibuprofen using this methodology,

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