Palladium-Catalyzed Base-Promoted Arylation of Unactivated C(sp3)–H Bonds by Aryl Iodides: A Practical Approach To Synthesize β-Aryl Carboxylic Acid Derivatives

Article abstract of DOI:10.1002/ejoc.201701215

A highly efficient protocol for the β-arylation of carboxylic amides by aryl iodides under PdCl₂(CH₃CN)₂/CsOAc catalysis was developed. This method was found to tolerate a broad scope of substrates and was successfully employed in the preparation of a variety of β-aryl α-amino and γ-amino acid derivatives. The utility of this method was further illustrated in the synthesis of the psychotropic drug (±)-phenibut and β-aryl bile acid analogues.