Wilkovitsch, M., Svatunek, D., Mikula, H., & Denk, C. (2023). Post-radiolabeling thioether oxidation to enhance the bioorthogonal reactivity of 18F-tetrazines. MONATSHEFTE FUR CHEMIE, 154(12), 1441–1457. https://doi.org/10.1007/s00706-023-03140-w
Radiolabeled 1,2,4,5-tetrazines are powerful heterocyclic agents for bioorthogonal PET imaging due to their fast cycloaddition with trans-cyclooctenes. However, fluorine-18 radiolabeling of highly reactive tetrazines is often not feasible due to limited compound stability. We demonstrate that post-radiolabeling oxidation of thioether functionalities is a viable and transferable strategy to avoid these limitations, enabling the synthesis of highly reactive 18F-tetrazines.
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Research facilities:
TRIGA Mark II-Nuklearreaktor Zentrum für Kernspinresonanzspektroskopie
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Project title:
In Vivo Klick für PET": Verbesserung der Diagnose in der klinischen Nanomedizin: 668532 (European Commission)