Pd(II)-Catalyzed Strategies for the β-Arylation of α-AminoAcids: An Overview

Metal-catalyzed C─H activation has been linked to amino acidsfor decades. Peptides and α-amino acids (α-AAs) have beenused as substrates, directing groups (DGs) and ligands, signif-icantly expanding and broadening the definition of metallo-and organo-catalysis. This mini-review focuses on strategiesfor β-arylation of α-AAs involving Pd(II)-mediated activation ofthe β-C(sp 3 )-H sigma bond. After a brief introduction in Sec-tion 1, strategies exploiting auxiliary bidentate DGs to addressthe Pd(II)-mediated C─H activation are discussed in Section2. The related Ligand-controlled processes are treated in Sec-tion 3 and Section 4 highlight the most recent atom-economicdevelopments in peptide late-stage functionalization (LSF) pro-ceeding via Pd(II)-mediated β-C(sp 3 )-H activation of a preciseα-AA residue along the peptide sequence