用于快速高效[18 F]氟化物干燥的开源流程设置,实现 PET 示踪剂合成自动化。

IF 0.9 4区 医学 Q4 BIOCHEMICAL RESEARCH METHODS Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-12-28 DOI:10.1002/jlcr.4080
Florian Menzel, Jonathan Cotton, Thomas Ziegler, Andreas Maurer, Jochen M. Neumaier
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引用次数: 0

摘要

放射化学研究设施的关键战略之一是实现合成过程的自动化。不必要的人工操作会增加工作人员的辐射暴露,同时威胁合成的可靠性。我们曾报道过一种经济实惠的开源系统,该系统由 3D 打印连续流反应器、定制注射泵和压力调节器组成,可用于进行放射性氟化。在本文中,我们将讨论放射性示踪剂开发和合成所需的其他基本流程,目的是使实验室工作更安全、研究更高效。我们设计并评估了一种可直接连接回旋加速器的全自动系统,用于快速有效地处理和干燥[18 F]氟化物水溶液。该工艺依赖于三氟化丙烯气体的生成,可在 10 分钟内在热电池中安全制备亲核[18 F]氟化物,活性回收率为 91.7 ± 1.6% (n = 5)。由于需要方便的放射性氟化人工配体,我们对连续流动系统进行了调整,以制备[18 F]fluoroethyl tosylate (FEOTs)和[18 F]fluoroethyl triflate (FEOTf),这些人工基团被广泛用于 PET 示踪剂的后期氟乙基化。本文对不同基团的过程和放射性标记进行了比较和全面的讨论。快速高效地提供[18 F]氟乙基对甲苯磺酸盐(FEOTs)和[18 F]氟乙基三氟酯(FEOTf)的方法有利于放射化学研究。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Open-source flow setup for rapid and efficient [18F]fluoride drying for automation of PET tracer syntheses

One of the key strategies for radiochemical research facilities is the automation of synthesis processes. Unnecessary manual operations increase the radiation exposure of personnel, while simultaneously threatening the reliability of syntheses. We have previously reported an affordable open-source system comprising 3D-printed continuous flow reactors, a custom syringe pump, and a pressure regulator that can be used to perform radiofluorinations. In this paper, we address additional essential processes that are needed for radiotracer development and synthesis, with the aim of making laboratory work safer and research more efficient. We have designed and evaluated a fully automated system for rapidly and effectively processing and drying aqueous [18F]fluoride that can be directly connected to the cyclotron. This process relies on triflyl fluoride gas generation and allows nucleophilic [18F]fluoride to be prepared safely in a hotcell within 10 min and an activity recovery of 91.7 ± 1.6% (n = 5). Owing to the need for convenient radiofluorinated prosthetic ligands, we have adapted our continuous flow system to produce [18F]fluoroethyl tosylate (FEOTs) and [18F]fluoroethyl triflate (FEOTf), prosthetic groups that are widely used for late-stage fluoroethylation of PET tracers. The processes as well as the radiolabeling of different groups are compared and comprehensively discussed. Having a method providing [18F]fluoroethyl tosylate (FEOTs) as well as [18F]fluoroethyl triflate (FEOTf) quickly and highly efficiently is beneficial for radiochemical research.

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来源期刊
CiteScore
3.30
自引率
0.00%
发文量
57
审稿时长
1 months
期刊介绍: The Journal of Labelled Compounds and Radiopharmaceuticals publishes all aspects of research dealing with labeled compound preparation and applications of these compounds. This includes tracer methods used in medical, pharmacological, biological, biochemical and chemical research in vitro and in vivo. The Journal of Labelled Compounds and Radiopharmaceuticals devotes particular attention to biomedical research, diagnostic and therapeutic applications of radiopharmaceuticals, covering all stages of development from basic metabolic research and technological development to preclinical and clinical studies based on physically and chemically well characterized molecular structures, coordination compounds and nano-particles.
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