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

Metal-catalyzed C─H activation has been linked to amino acids for decades. Peptides and $\alpha$ -amino acids (α-AAs) have been used as substrates, directing groups (DGs) and ligands, significantly expanding and broadening the definition of metallo- and organo-catalysis. This mini-review focuses on strategies for β-arylation of α-AAs involving Pd(II)-mediated activation of the β-C(sp³)-H sigma bond. After a brief introduction in Section 1, strategies exploiting auxiliary bidentate DGs to address the Pd(II)-mediated C─H activation are discussed in Section 2. The related Ligand-controlled processes are treated in Section 3 and Section 4 highlight the most recent atom-economic developments in peptide late-stage functionalization (LSF) proceeding via Pd(II)-mediated β-C(sp³)-H activation of a precise $\alpha$ -AA residue along the peptide sequence.