We have developed a method for auxiliary-directed, palladium-catalyzed β-arylation and alkylation of sp3 and sp2 C− H bonds in carboxylic acid derivatives. The method employs a carboxylic acid 2-methylthioaniline-or 8-aminoquinoline amide substrate, aryl or alkyl iodide coupling partner, palladium acetate catalyst, and an inorganic base. By employing 2- methylthioaniline auxiliary, selective monoarylation of primary sp3 C− H bonds can be ...