[18F]氟咪唑合成方法的开发与优化

IF 1.4 3区 化学 Q4 CHEMISTRY, INORGANIC & NUCLEAR
Maja Chochevska, Marija Atanasova Lazareva, Katerina Kolevska, Maja Velichkovska, J. Koziorowski, E. Ivanovska, B. Angelovska, A. Ugrinska
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引用次数: 0

摘要

摘要[18F]氟味噌硝唑([18F]FMISO)作为硝基咪唑衍生物与18F放射性同位素是一种广泛已知和研究的PET成像缺氧标志物。近年来,已经描述了用于生产[18F]FMISO的许多自动化合成模块和纯化策略。这项工作的目标是开发[18F]FMISO合成工艺,使用带有固相萃取(SPE)Sep-Pak纯化筒的Synthera模块。为了调整反应条件,我们在不同的反应条件下合成了[18F]FMISO,并使用各种反相(RP)纯化盒(HLB-light,HLB-plus,tC18,C18 environmental,Chromafix PS-RP)。通过商业1-(2′-硝基-1′-咪唑基)-2-O-四氢吡喃基-3-O-甲苯磺酰基丙二醇前体的亲核取代和随后的酸性水解进行合成。此外,通过使产物混合物通过SPE筒进行纯化。产生的[18F]FMISO保留在滤筒上,而杂质通过滤筒进入废物中。然后用少量乙醇在水中洗脱保留的[18F]FMISO,并将洗脱液收集在最终产品小瓶中。产品样品进行了质量控制测试,而废物样品则进行了化学和放射化学测试。我们根据欧洲药典关于氟甲硝唑(18F)注射液的专论,开发了一种高效的[18F]FMISO的筒式纯化合成方法,该方法具有良好的放射化学产率(RCY)和高的化学和放射化学纯度。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
[18F]Fluoromisonidazole synthesis method: development and optimization by cartridge purification
Abstract [18F]Fluoromisonidazole ([18F]FMISO) as nitroimidazole derivative with 18F radioisotope is a widely known and studied hypoxia marker for PET imaging. A number of automated synthesis modules and purification strategies for production of [18F]FMISO have been described in recent years. The goal of this work was to develop [18F]FMISO synthesis process with Synthera module with solid phase extraction (SPE) Sep-Pak purification cartridges. To adjust the reaction conditions we synthesized [18F]FMISO under different reaction conditions and using various reversed-phase (RP) purification cartridges (HLB light, HLB plus, tC18, C18 environmental, Chromafix PS-RP). The synthesis was performed by nucleophilic substitution of commercial 1-(2′-nitro-1′-imidazolyl)-2-O-tetrahydropyranyl-3-O-toluenesulfonylpropanediol precursor and subsequent acidic hydrolysis. Further, the product mixture was purified by passing through the SPE cartridge. The produced [18F]FMISO was retained on the cartridge, while the impurities passed through the cartridge into a waste. The retained [18F]FMISO was then eluted with small amounts of ethanol in water and eluates were collected in the final product vial. The product sample was subjected to quality control tests, while for waste sample chemical and radiochemical tests were performed. We have developed an efficient synthesis method of [18F]FMISO with cartridge purification with good radiochemical yield (RCY) and high chemical and radiochemical purity in accordance with the Ph. Eur. Monograph for Fluoromisonidazole (18F) injection.
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来源期刊
Radiochimica Acta
Radiochimica Acta 化学-核科学技术
CiteScore
2.90
自引率
16.70%
发文量
78
审稿时长
6 months
期刊介绍: Radiochimica Acta publishes manuscripts encompassing chemical aspects of nuclear science and technology.
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