Metal Catalysis within Tyrosine Bioconjugation

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.