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A novel prosthetic group for the efficient radiolabeling of macromolecules has been developed. [ 18 F]oxadibenzocyclooctyne ([ 18 F]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.

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

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