Pd‐Catalyzed CH Oxygenation with TFA/TFAA: Expedient Access to Oxygen‐Containing Heterocycles and Late‐Stage Drug Modification

Abstract

Acid brings the oxygen: a general method for palladium-catalyzed C-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-H activation.