Site-selective and diastereoselective functionalization of α-amino acid and peptide derivatives via palladium-catalyzed sp3 C-H activation

alpha-Amino acid and peptide derivatives are important in synthetic organic chemistry and medicinal chemistry, which attract many chemists to develop new methods for their synthesis. Palladium-catalyzed sp(3) C-H activation/functionalization has been developed greatly for the modification of alpha-amino acids and peptides. This review introduces palladium-catalyzed sp(3) C-H activation/functionalization of amino acids and peptides. The content includes intermolecular functionalization (arylation, alkylation, alkenylation, alkynylation, acetoxylation, fluorination, silylation, borylation, sulfonylation, chalcogenation and carbonylative cyclization) and intramolecular functionalization (intramolecular C-N bond-forming cyclization and peptide macrocyclization).

Automated summary

This review discusses the palladium-catalyzed sp(3) C-H activation/functionalization of amino acids and peptides, including intermolecular and intramolecular functionalization methods.