在铜介导的放射性化中化的副作用反应
Sarandeep Kaur1,2, Barbara Wenzel3, Ramona Oehme4
1Department of Experimental Neurooncological Radiopharmacy, Helmholtz-Zentrum Dresden-Rossendorf (HZDR), Institute of Radiopharmaceutical Cancer Research, 04318, Leipzig, Germany. s.kaur@hzdr.de.
这项研究通过确定关键参数来最大限度地减少化副产品 (HSP) 来优化铜介导放射性化 (CMRF). 微调反应条件和前体选择显著减少HSP的形成,改善放射性追踪剂的产生.
科学领域:
- 放射化学 放射化学是指辐射化学.
- 有机合成 有机合成
- 药用化学 医学化学
背景情况:
- 铜介导放射化 (CMRF) 是将-18纳入分子中的一个关键技术.
- 导致化副产品 (HSP) 的原体化仍然是CMRF的一个重大挑战.
- 高酸的形成使放射性追踪剂的净化和生产复杂化.
研究的目的:
- 研究影响CMRF中化反应速率的因素.
- 确定CMRF过程中的原始脱过程中的来源.
- 优化CMRF协议以最大限度地减少HSP的形成,并增强放射化学转换 (RCC).
主要方法:
- 使用的模型前体具有各种脱离组 (-B(OH) 2, -Bpin, -BEpin, -SnBu3).
- 系统地改变化学成分 (反应剂类型/分子量) 和物理参数 (时间,温度).
- 使用化试剂和高分辨率质谱 (HRMS) 来追踪的起源.
主要成果:
- 确定了显著影响HSP形成率的反应参数.
- 确定了最佳条件:低温,短反应时间,最小的前体/铜,没有和酒精.
- -BEpin前体产生的HSP最低,而 -B(OH) 2前体产生的最高.
- 确定精心选择试剂和微调参数可以减少HSP的形成.
结论:
- 反应参数优化和前体选择对于最小化CMRF中的HSP至关重要.
- 实现了高放射化学转化 (RCC),显著减少了HSP的形成.
- 这项研究为使用CMRF的更有效,更可靠的放射追踪器生产提供了框架.
更多相关视频
10:10Application of Elemental Lanthanides in the Selective C-F Activation of Trifluoromethylated Benzofulvenes Providing Access to Various Difluoroalkenes
Published on: July 28, 2018
09:35Preparation of a Corannulene-functionalized Hexahelicene by CopperI-catalyzed Alkyne-azide Cycloaddition of Nonplanar Polyaromatic Units
Published on: September 18, 2016
相关概念视频
Electrophilic Aromatic Substitution: Fluorination and Iodination of Benzene
Radical Substitution: Hydrogenolysis of Alkyl Halides with Tributyltin Hydride
The bonds formed in this reaction are stronger than the bonds broken, making it energetically favorable. The reaction follows a radical chain mechanism similar to radical halogenation reactions,...
Halogenation of Alkenes
Consider the bromination of cyclopentene. Molecular bromine is polarized in the proximity of the π electrons of cyclopentene. An electrophilic bromine atom adds across the double bond, forming a cyclic bromonium ion intermediate.
Reduction of Alkenes: Catalytic Hydrogenation
Metals like palladium, platinum, and nickel are commonly used in their solid forms — fine powder on an inert surface. As these catalysts remain insoluble in the reaction mixture, they are referred to as heterogeneous catalysts.
The hydrogenation process takes place on the...
Base-Promoted α-Halogenation of Aldehydes and Ketones
Reduction of Alkynes to cis-Alkenes: Catalytic Hydrogenation
Like alkenes, alkynes can be reduced to alkanes in the presence of transition metal catalysts such as Pt, Pd, or Ni. The reaction involves two sequential syn additions of hydrogen via a cis-alkene intermediate.
![[DPEPhosbcpCu]PF6: A General and Broadly Applicable Copper-Based Photoredox Catalyst](/_next/image?url=https%3A%2F%2Fcloudfront.jove.com%2FCDNSource%2Fteasers%2F59739.jpg&w=3840&q=50)