[F]二碳素用于正电子发射断层扫描
Jeroen B I Sap1, Claudio F Meyer1,2, Joseph Ford1
1University of Oxford, Chemistry Research Laboratory, Oxford, UK.
Nature
|March 28, 2022
概括
研究人员开发了一种新的-18二碳酸试剂,用于高效的放射性标记. 这一突破使得高分子活性二甲基化成为药物发现和分子成像应用的关键.
科学领域:
- 核成像技术
- 放射化学
- 有机合成
背景情况:
- 全身正子发射断层扫描 (PET) 扩展了分子成像研究.
- -18 (F) 放射化学已经进步,但F-二甲基化仍然具有挑战性.
- 二甲基对药物发现至关重要.
研究的目的:
- 引入F-二甲基化的一般溶液.
- 开发用于核成像的多功能二碳酸试剂.
- 为了能够对二甲基化分子进行高分子活性标记.
主要方法:
- 用于核成像应用的碳素化学.
- 设计了一种新的二碳酸试剂,
- 对前体电子的同位素稀释效应进行了研究.
- 通过O-H,S-H和N-H插入和交叉合反应证明了多功能性.
主要成果:
- 开发了一种用于F-二甲基化的通用溶液.
- 获得高活动标记.
- 显示了各种功能组的试剂多功能性,包括 (thio) ,N-heteroarenes和酸.
- 成功标记了复杂的生物相关分子和放射性标记物.
结论:
- 新的二碳酸试剂克服了以前在二甲基化中的局限性.
- 这种方法可以很容易地获得高分子活性二甲基化合物.
- 该试剂的多功能性和影响性在用于PET成像和药物发现的复杂分子标记中得到证明.
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