硫[18F]化物交换 点击化学 启用超快速后期放射合成
Qinheng Zheng1, Hongtao Xu2, Hua Wang1,3
1Department of Chemistry, The Scripps Research Institute, La Jolla, California 94037, United States.
Journal of the American Chemical Society
|February 25, 2021
概括
我们开发了一种超快速的放射合成, 这种快速方法可为体内成像应用提供高效的放射性标记和净化.
科学领域:
- 放射化学
- 医学化学
- 核医学
背景情况:
- 有效的[18F]化方法对于开发新型正电子发射断层扫描 (PET) 剂至关重要.
- 针对PET成像的特定有机化合物的合成仍然是一个重大挑战.
研究的目的:
- 开发一种超快速的同位素交换方法,用于新型酸PET剂的放射合成.
- 为了利用硫化物交换 (SuFEx) 快速进行18F放射性标记.
主要方法:
- 使用SuFEx点击化学方法进行超快的同位素交换反应.
- 该方法应用于对25种不同酸的自动化18F放射性标记.
- 通过简单的片过来实现净化,避免使用HPLC.
主要成果:
- 在室温下在30秒内获得了优异的放射性化学产量 (83-100%,中位数98%) 和高分子活性 (280GBq/μmol).
- 该方法在25种结构不同的基酸盐中显示出广泛的适用性.
- 使用PARP1向剂,成功实现了皮下瘤的体内成像.
结论:
- 开发的基于SuFEx的放射合成提供了一种高效和快速的方法来产生新型的18F酸PET剂.
- 这种方法克服了[18F]化方面的局限性,并促进了新的诊断工具的开发.
- 这种方法对体内分子成像具有前景,以PARP1向研究为例.
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