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

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.