β-Hydroxy carbonyl scaffolds are of paramount importance due to their presence in a variety of natural products and bioactive molecules. In this study, we present a direct palladium-catalyzed β-C(sp3)–H hydroxylation of aliphatic carboxylic acids. The reported method employs convenient and readily available TBHP as an oxidant and provides an efficient, one-step route to a diverse range of β-hydroxy acids. Key aspects include the compatibility of this method with challenging α-non-quaternary carboxylic acids as substrates and excellent functional group tolerance. This newly developed method is expected to prove useful for generating compound libraries relevant to multiple disciplines.

A direct palladium-catalyzed γ-lactonization of free carboxylic acids via C–O reductive elimination as a key step is described. Notable aspects of this protocol include the use of convenient and easil...