The Bioorthogonal Chemistry for Development of Novel Radiopharmaceuticals

Bioorthogonal chemistry defines chemical reactions that selectively occur within living organisms without interacting with other biological processes, establishing itself as a useful tool in the development of radiopharmaceuticals. These reactions are characterized by high selectivity, allowing them to occur selectively between designated molecules and biocompatibility in aqueous conditions. In this review, we explain representative bioorthogonal reactions, such as Copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC), strain-promoted azide-alkyne cycloaddition (SPAAC), the inverse electron demand Diels-Alder reaction (iEDDA) utilizing tetrazine and trans-cyclooctene, and the Staudinger ligation and discuss development of novel radiopharmaceuticals based on these reactions.