Synthesis Principle and Practice with Radioactive Iodines and Astatine: Advances Made So Far,The Journal of Organic Chemistry

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Synthesis Principle and Practice with Radioactive Iodines and Astatine: Advances Made So Far
The Journal of Organic Chemistry ( IF 3.3 ) Pub Date : 2024-08-22 , DOI: 10.1021/acs.joc.4c00593
Taotao Dong _{1,

2} , Zhenru Zhang _{1,

2} , Weicai Li _{1,

2} , Weibin Zhuo ₃ , Tongjiang Cui ₃ , Zijing Li _{1,

2}

Affiliation

Radioactive iodines and astatine, possessing distinct exploitable nuclear properties, play indispensable roles in the realms of nuclear imaging and therapy. Their analogous chemical characteristics shape the design, preparation, and substrate range for tracers labeled with these radiohalogens through interconnected radiosynthetic chemistry. This perspective systematically explores the labeling methods by types of halogenating reagents─nucleophilic and electrophilic─underpinning the rational design of such compounds. It delves into the rapidly evolving synthetic strategies and reactions in radioiodination and radioastatination over the past decade, comparing their intrinsic relationships and highlighting variations. This comparative analysis illuminates potential radiosynthetic methods for exploration. Moreover, stability concerns related to compounds labeled with radioactive iodines and astatine are addressed, offering valuable insights for radiochemists and physicians alike.

中文翻译：

放射性碘和砹的合成原理与实践：迄今为止取得的进展

放射性碘和砹具有独特的可利用核特性，在核成像和治疗领域发挥着不可或缺的作用。它们类似的化学特性决定了通过相互关联的放射合成化学用这些放射性卤素标记的示踪剂的设计、制备和底物范围。这一观点系统地探索了卤化试剂类型（亲核试剂和亲电子试剂）的标记方法，为此类化合物的合理设计奠定了基础。它深入研究了过去十年中放射性碘化和放射性砹化的快速发展的合成策略和反应，比较了它们的内在关系并强调了变化。这种比较分析阐明了潜在的放射合成方法的探索。此外，还解决了与放射性碘和砹标记的化合物相关的稳定性问题，为放射化学家和医生等提供了宝贵的见解。

更新日期：2024-08-22

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