用于选择性S-18F和C-18F键形成的2,2-difluorovinyl动机中受控反应性转移的协议
Mudasir Maqbool1,2, Jimmy Erik Jakobsson1, Santosh Reddy Alluri1
1Department of Clinical Neurocience, OUS-Ullevål, Oslo, Norway.
Communications chemistry
|April 29, 2024
概括
一种新方法使得可用于正子发射断层扫描 (PET) 成像的高效射线追踪器产生. 这种技术利用选择性C-F键形成来开发新的诊断和治疗药物.
科学领域:
- 放射化学 放射化学是指辐射化学.
- 医疗成像医学成像
- 有机合成 有机合成
背景情况:
- 阳位子发射断层扫描 (PET) 依赖于放射标志物用于体内成像.
- -18是PET放射追踪器发展的关键正子发射器.
- 有效和选择性的放射性标记方法对于推进PET应用至关重要.
研究的目的:
- 开发一种新的,高效的,选择性的辐射追踪剂合成协议.
- 为了使易于生产-18标记化合物.
- 为了促进新的PET成像剂的临床翻译.
主要方法:
- 通过激活1,1-二乙烯基组来形成C-F键的新协议.
- 选择性氧化或减少策略用于键形成.
- 在日常生产中使用温和且无异议的化学试剂.
主要成果:
- 放射性追踪剂的高产量和标签试剂2,2-二二二-18F) 乙基4-甲基硫酸盐 ([18F]1b).
- 通过氧化成功合成硫尼尔化物作为初级产品.
- 证明了一种放射测定方法的原理证明,以量化硫化.
结论:
- 开发的方法为放射性标记提供了操作方便和温和的条件.
- 对生物分子,酶抑制剂和温度敏感化合物的标记具有很高的潜力.
- 促进了新PET放射追踪剂的临床转化.
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