Rh(I)-Catalyzed Direct C6-H Arylation of 2-Pyridones with Aryl Carboxylic Acids

A Rh(I)-catalyzed C6-selective C-H arylation of 2-pyridones with inexpensive, readily available, safe and structurally diverse aryl carboxylic acids with the aid of a pyridine directing group is developed. This decarbonylative arylation protocol features an easy-to-handle catalytic system, and is amenable to diversely substituted 2-pyridones and aryl carboxylic acids. It allows access to a wide range of C6-arylated 2-pyridones, including those that are difficult to prepare using conventional C-H arylation processes. The method tolerates various electron-neutral, electron-rich and electron-deficient functional groups, and affords the products in 41-91% yields.

Automated summary

The method employs inexpensive, readily available, and safe aryl carboxylic acids with a pyridine directing group to achieve C6-selective C-H arylation, allowing for a wide range of substituted 2-pyridones and affording products in yields of 41-91%.