Ligand-Enabled Scalable C-H Hydroxylation of Benzoic and Phenylacetic Acids at Room Temperature
Summary
The USPTO published patent application US20260092029A1 by Yu/Quan et al. disclosing methods for Pd-catalyzed C-H hydroxylation of benzoic and phenylacetic acids at room temperature using bifunctional pyridone-carboxylic acid ligands and aqueous hydrogen peroxide as oxidant. The application, filed September 7, 2023, also covers synthesis of polyfluorinated natural products and ibuprofen hydroxylation.
What changed
The USPTO published patent application US20260092029A1 disclosing ligand-enabled scalable methods for room-temperature palladium-catalyzed C-H hydroxylation of benzoic and phenylacetic acids. The key technical advance involves using bifunctional bidentate pyridone-carboxylic acid ligands (e.g., 2-methyl-2-(6-oxo-1,6-dihydropyridin-2-yl)propanoic acid) with aqueous hydrogen peroxide as an industry-compatible oxidant. The application covers derivatization methods, synthesis of polyfluorinated natural products (coumestan, pterocarpene) from phenol building blocks, and hydroxylation of ibuprofen.
Patent application publications are informational notices; no immediate action is required from chemical or pharmaceutical companies. Research and development teams should review the disclosed synthetic methodology for potential licensing evaluation or to assess freedom-to-operate implications. The application number is 19109042.
Archived snapshot
Apr 2, 2026GovPing captured this document from the original source. If the source has since changed or been removed, this is the text as it existed at that time.
LIGAND-ENABLED SCALABLE C-H HYDROXYLATION OF BENZOIC AND PHENYLACETIC ACIDS AT ROOM TEMPERATURE
Application US20260092029A1 Kind: A1 Apr 02, 2026
Inventors
Jin-Quan YU, Zhen LI, Han Seul PARK
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 CāH 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,
CPC Classifications
C07C 51/367 C07D 235/12 C07D 263/14 C07D 307/83 C07D 307/84 C07D 311/18 C07D 493/04 C07J 1/0059
Filing Date
2023-09-07
Application No.
19109042
Named provisions
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