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Pd-Catalyzed C[BOND]H Oxygenation with TFA/TFAA: Expedient Access to Oxygen-Containing Heterocycles and Late-Stage Drug Modification

Authors

  • Gang Shan,

    1. Department of Pharmacology and Pharmaceutical Sciences, School of Medicine and School of Life Sciences, Tsinghua University, Beijing, 100084 (China)
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  • Xinglin Yang,

    1. Department of Pharmacology and Pharmaceutical Sciences, School of Medicine and School of Life Sciences, Tsinghua University, Beijing, 100084 (China)
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  • Linlin Ma,

    1. Department of Pharmacology and Pharmaceutical Sciences, School of Medicine and School of Life Sciences, Tsinghua University, Beijing, 100084 (China)
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  • Prof. Dr. Yu Rao

    Corresponding author
    1. Department of Pharmacology and Pharmaceutical Sciences, School of Medicine and School of Life Sciences, Tsinghua University, Beijing, 100084 (China)
    • Department of Pharmacology and Pharmaceutical Sciences, School of Medicine and School of Life Sciences, Tsinghua University, Beijing, 100084 (China)
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  • This work was supported by a national “973” grant (2011CB965300), an NSFC grant (21142008), Tsinghua University 985 Phase II funds, and the Tsinghua University Initiative Scientific Research Program. TFA=trifluoroacetic acid, TFAA=trifluoroacetic anhydride.

Abstract

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Acid brings the oxygen: A general method for palladium-catalyzed C[BOND]H oxygenation has been developed for the facile synthesis of a wide range of functionalized phenols with readily available aryl ketones, benzoates, benzamides, acetanilides, and sulfonamides. A trifluoroacetic acid/trifluoroacetic acid anhydride solvent system serves as the oxygen source and is the critical factor for C[BOND]H activation.

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