氮杂环卡宾介导的协同芳香亲核取代在18F标记反应中的应用进展

Application Progress of N-Heterocyclic Carbene-mediated Concerted Nucleophilic Aromatic Substitution in 18F Labeling Reaction

  • 摘要: 协同芳香亲核取代反应(CSNAr)在核化学合成中具有十分重要的地位,该反应现今可用于开发正电子放射性示踪剂。相较于传统的芳香亲核取代反应,CSNAr的反应底物范围不局限于缺电子芳烃,以及放射性标记的产物可以方便地从反应体系中分离出来。本研究首先阐述了协同芳香亲核取代反应的机理,重点阐述了1,3-双(2,6-二异丙基苯基)2-氯咪唑鎓氯盐(SIPr·HCl)介导的CSNAr反应及其在正电子核素标记放射性示踪剂制备中的应用进展。最后强调了协同芳香亲核取代反应对合成18F放射性示踪剂的重要性,总结存在的不足,展望未来应用前景。

     

    Abstract: Concerted nucleophilic aromatic (CSNAr) substitution reactions play an important role in nuclear chemistry synthesis, and are now used to develop positron radiotracers. Compared with the traditional nucleophilic aromatic substitution reaction, the advantages of this substitution reaction lie in the fact that the range of substrates is not limited to electron-deficient aromatic compounds, and the radiolabeled products can be easily separated from the reaction system. In this paper, the mechanism of concerted nucleophilic aromatic substitution reaction was first elaborated, and the CSNAr reaction mediated by 1,3-bis(2,6-diisopropylphenyl)2-chloroimidazolium chloride(SIPr·HCl) and its application progress in the preparation of positron nuclide-labeled radiotracer were focused. We emphasized the importance of concerted nucleophilic aromatic substitution reactions for synthesizing 18F radiotracers, summarized existing shortcomings, and prospectd future application prospects.

     

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