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 ‐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(sp 3 )‐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(sp 3 )‐H activation of a precise ‐AA residue along the peptide sequence.