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.

Graphical abstract

中文翻译：

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放射性标记后硫醚氧化增强 18F-四嗪的生物正交反应活性

放射性标记的 1,2,4,5-四嗪是用于生物正交 PET 成像的强大杂环试剂，因为它们能够与反式环辛烯快速环加成。然而，由于化合物稳定性有限，高活性四嗪的氟 18 放射性标记通常不可行。我们证明硫醚官能团的放射性标记后氧化是避免这些限制的可行且可转移的策略，从而能够合成高反应性的¹⁸ F-四嗪。

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