Pd(ii)-catalyzed alkylation of unactivated C(sp3)–H bonds: efficient synthesis of optically active unnatural α-amino acids

A palladium-catalyzed alkylation of primary and secondary C(sp3)–H bonds with alkyl iodides and/or bromides for the synthesis of optically active unnatural α-amino acids (α-AAs) is described. This process is scalable and tolerates a variety of functional groups with complete retention of chirality, providing an efficient new strategy for the synthesis of various unnatural α-amino acid derivatives.