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无需对氟-18进行共沸干燥即可在室温下简便合成氟-18标记的氟烟酸-2,3,5,6-四氟苯酯。

Facile room temperature synthesis of fluorine-18 labeled fluoronicotinic acid-2,3,5,6-tetrafluorophenyl ester without azeotropic drying of fluorine-18.

作者信息

Basuli Falguni, Zhang Xiang, Jagoda Elaine M, Choyke Peter L, Swenson Rolf E

机构信息

Imaging Probe Development Center, National Heart, Lung, and Blood Institute, National Institutes of Health, Rockville, MD.

Imaging Probe Development Center, National Heart, Lung, and Blood Institute, National Institutes of Health, Rockville, MD.

出版信息

Nucl Med Biol. 2016 Dec;43(12):770-772. doi: 10.1016/j.nucmedbio.2016.08.008. Epub 2016 Aug 30.

Abstract

Fluorine-18 labeled fluoronicotinic acid-2,3,5,6-tetrafluorophenyl ester has been successfully synthesized in an unprecedented way by flowing an acetonitrile solution of its quaternary ammonium salt precursor (N,N,N-trimethyl-5-((2,3,5,6-tetrafluorophenoxy)carbonyl)pyridin-2-aminium trifluoromethanesulfonate, 1) through an anion exchange cartridge. The fluorination reaction proceeded at room temperature without azeotropic drying of the fluoride. Over 75% conversion was observed with 10mg of precursor in 2:8, acetonitrile: t-butanol in 1min. The total synthesis time was 5min which is ~30min shorter than the current literature method.

摘要

通过使其四元铵盐前体(N,N,N-三甲基-5-((2,3,5,6-四氟苯氧基)羰基)吡啶-2-氨基三氟甲磺酸盐,1)的乙腈溶液流经阴离子交换柱,以一种前所未有的方式成功合成了氟-18标记的氟烟酸-2,3,5,6-四氟苯酯。氟化反应在室温下进行,无需对氟化物进行共沸干燥。在1分钟内,10毫克前体在乙腈与叔丁醇体积比为2:8的混合溶剂中反应,转化率超过75%。总合成时间为5分钟,比目前文献方法短约30分钟。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/db48/5118155/80fb68713467/nihms-814039-f0001.jpg

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