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钯介导的(18)F-氟代在正电子发射断层扫描放射性示踪剂开发中的应用:克服转化障碍。

Application of palladium-mediated (18)F-fluorination to PET radiotracer development: overcoming hurdles to translation.

机构信息

Department of Chemistry and Chemical Biology, Harvard University, Cambridge, MA, USA.

出版信息

PLoS One. 2013;8(3):e59187. doi: 10.1371/journal.pone.0059187. Epub 2013 Mar 12.

Abstract

New chemistry methods for the synthesis of radiolabeled small molecules have the potential to impact clinical positron emission tomography (PET) imaging, if they can be successfully translated. However, progression of modern reactions from the stage of synthetic chemistry development to the preparation of radiotracer doses ready for use in human PET imaging is challenging and rare. Here we describe the process of and the successful translation of a modern palladium-mediated fluorination reaction to non-human primate (NHP) baboon PET imaging-an important milestone on the path to human PET imaging. The method, which transforms [(18)F]fluoride into an electrophilic fluorination reagent, provides access to aryl-(18)F bonds that would be challenging to synthesize via conventional radiochemistry methods.

摘要

新的化学方法可用于合成放射性标记的小分子,如果能够成功转化,它们有可能对临床正电子发射断层扫描(PET)成像产生影响。然而,将现代反应从合成化学开发阶段推进到准备用于人类 PET 成像的放射性示踪剂剂量的阶段是具有挑战性且罕见的。在这里,我们描述了一种现代钯介导的氟化反应转化为非人类灵长类动物(NHP)狒狒 PET 成像的过程,这是人类 PET 成像道路上的重要里程碑。该方法将[(18)F]氟化物转化为亲电氟化试剂,可获得通过常规放射化学方法难以合成的芳基-(18)F 键。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7ca8/3595243/b68e29caff6f/pone.0059187.g001.jpg

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