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(sp(3))-H bonds with alkyl iodides and/or bromides for the synthesis of optically active unnatural alpha-amino acids (alpha-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 alpha-amino acid derivatives.