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核性18F-化异芳盐,没有添加载体[18F]化物
Tobias L Ross1, Johannes Ermert, Carsten Hocke
1Institut für Nuklearchemie, Forschungszentrum Jülich GmbH, D-52425 Jülich, Germany.
Journal of the American Chemical Society
|June 1, 2007
概括
具有2 - 乙烯基组的二利盐能够强烈的,区域选择性的无载体添加的化. 这种方法允许将[18F]化物单步核性引入到富含电子的中.
科学领域:
- 放射化学 放射化学是指辐射化学.
- 有机化学 有机化学
- 异环化学 异环化学
背景情况:
- 迪亚利盐是放射性化中的有效前体.
- 富含电子的异质芳香成分,如2 - 乙基,增强了反应性.
- 核性,无载体添加 (nca) 放射性化对于放射性药物开发至关重要.
研究的目的:
- 为了研究含有2-烯基组的二利盐作为nca放射性化前体.
- 探索将nca [18F]化物引入各种领域的区域选择性和效率.
- 了解替代模式,对应物和反应条件对放射性化过程的影响.
主要方法:
- 用系统变化的替代剂合成和应用2-2--盐.
- 研究反应动力学和与哈梅特常数的相关性.
- 研究对离子对的分离和反应性对抗离子和溶剂的影响.
主要成果:
- 具有2 - 乙烯基组的二利盐是区域选择性nca放射性化的强有力的前体.
- 实现了nca [18F]化物的单阶段核友性引入到富电子的中.
- 反应速率与哈梅特常数线性相关,证实了具有高反应性和低选择性的核友芳香替代.
结论:
- 二二二盐对的nca放射性化非常有效.
- 反应通过核友芳香替代进行,受替代物的电子性质的影响.
- 这种方法为在放射性药物研究中引入[18F]化物提供了有价值的工具.
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