Ligand-Enabled β-C-H Arylation of α-Amino Acids Without Installing Exogenous Directing Groups

Herein we report acid-directed -C(sp(3))-H arylation of -amino acids enabled by pyridine-type ligands. This reaction does not require the installation of an exogenous directing group, is scalable, and enables the preparation of Fmoc-protected unnatural amino acids in three steps. The pyridine-type ligands are crucial for the development of this new C(sp(3))-H arylation.