Functionalization of aromatic amino acids via direct C-H activation: generation of versatile building blocks for accessing novel peptide space.

Functionalized α-amino acid building blocks have been prepared in good yield with high regiocontrol and preservation of stereochemistry via iridium-catalyzed borylation of suitably protected aromatic α-amino acid derivatives. The utility of these systems in peptide couplings and Suzuki reactions has been demonstrated.