[¹⁸F]ODIBO: a prosthetic group for bioorthogonal radiolabeling of macromolecules <i>via</i> strain-promoted alkyne–azide cycloaddition

Abstract

A novel prosthetic group for the efficient radiolabeling of macromolecules has been developed. [¹⁸F]oxadibenzocyclooctyne ([¹⁸F]ODIBO) is synthesized in high radiochemical yield and applied for nearly quantitative conjugation to azide-tagged peptides and proteins at room temperature and low substrate concentrations. The resulting bioconjugates are chemically and radiochemically pure and free of toxic solvents and catalysts.