Metal Catalysis within Tyrosine Bioconjugation

Abstract The post-modification of biomolecules in a late-stage fashion constitutes an unmet challenge of paramount importance within organic chemistry, drug discovery, and chemical biology. The functionalization of otherwise unreactive C–H bonds holds great promise for reducing the reliance on existing functional groups, thereby streamlining the chemical syntheses. Despite the extensive repertoire of peptide labelling techniques currently available, the site-selective modification of tyrosine (Tyr) compounds remains comparatively underexplored. This review highlights the state-of-the-art regarding the use of metal catalysis within the ortho-C–H functionalization of Tyr-containing compounds.