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[F] 乙烯磺酰氟作为一种实用的放射性氟化物中继试剂。

[ F]Ethenesulfonyl Fluoride as a Practical Radiofluoride Relay Reagent.

作者信息

Zhang Bo, Fraser Benjamin H, Klenner Mitchell A, Chen Zhen, Liang Steven H, Massi Massimiliano, Robinson Andrea J, Pascali Giancarlo

机构信息

Australian Nuclear Science and Technology Organisation (ANSTO), New Illawarra Rd., Lucas Heights, NSW, Australia.

Faculty of Science, Monash University, Wellington Rd., Clayton, Victoria, Australia.

出版信息

Chemistry. 2019 Jun 7;25(32):7613-7617. doi: 10.1002/chem.201900930. Epub 2019 May 9.

Abstract

Fluorine-18 is the most utilized radioisotope in positron emission tomography (PET), but the wide application of fluorine-18 radiopharmaceuticals is hindered by its challenging labelling conditions. As such, many potentially important radiotracers remain underutilized. Herein, we describe the use of [ F]ethenesulfonyl fluoride (ESF) as a novel radiofluoride relay reagent that allows radiofluorination reactions to be performed in minimally equipped satellite nuclear medicine centres. [ F]ESF has a simple and reliable production route and can be stored on inert cartridges. The cartridges can then be shipped remotely and the trapped [ F]ESF can be liberated by simple solvent elution. We have tested 18 radiolabelling precursors, inclusive of model and clinically used structures, and most precursors have demonstrated comparable radiofluorination efficiencies to those obtained using a conventionally dried [ F]fluoride source.

摘要

氟-18是正电子发射断层扫描(PET)中使用最广泛的放射性同位素,但氟-18放射性药物的广泛应用受到其具有挑战性的标记条件的阻碍。因此,许多潜在重要的放射性示踪剂仍未得到充分利用。在此,我们描述了使用[F]乙烯磺酰氟(ESF)作为一种新型放射性氟化物中继试剂,它能使放射性氟化反应在设备最少的卫星核医学中心进行。[F]ESF具有简单可靠的生产路线,并且可以储存在惰性药筒中。然后这些药筒可以远程运输,捕获的[F]ESF可以通过简单的溶剂洗脱释放出来。我们测试了18种放射性标记前体,包括模型结构和临床使用的结构,大多数前体已证明其放射性氟化效率与使用传统干燥[F]氟化物源获得的效率相当。

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