PET肿瘤显像剂18F-氟乙基胆碱的自动化合成

doi:10.7538/tws.2010.23.02.0081

同位素 ›› 2010, Vol. 23 ›› Issue (2): 81-85.DOI: 10.7538/tws.2010.23.02.0081

• 放射性药物和标记化合物 • 上一篇下一篇

PET肿瘤显像剂¹⁸F-氟乙基胆碱的自动化合成

党永红;李方;吕京桥;邢海群

中国医学科学院北京协和医学院，北京协和医院核医学科，北京100730

收稿日期:1900-01-01 修回日期:1900-01-01 出版日期:2010-05-20 发布日期:2010-05-20

Automatic Synthesis of Tumor Imaging Agent ¹⁸F-fluoroethylcholine

DANG Yong-hong; LI Fang; Lü Jing-qiao;XING Hai-qun

Department of Nuclear Medicine, PUMC Hospital， Peking Union Medical College & Chinese Academy of Medical Science, Beijing 100730, China

Received:1900-01-01 Revised:1900-01-01 Online:2010-05-20 Published:2010-05-20

摘要/Abstract

摘要： ¹⁸F-氟乙基胆碱（¹⁸F-FECH）是反映胆碱代谢的PET肿瘤显像剂，在肿瘤特别是脑肿瘤诊断中显示出良好的应用前景。为了方便临床应用，本工作利用PET-MF-2V-IT-I型¹⁸F多功能合成模块，自动化合成¹⁸F-FECH。首先¹⁸F^-与1,2-乙二醇二对甲苯磺酸酯在90 ℃下发生亲核取代反应，产物未经纯化即与N,N二甲基乙醇胺在100 ℃下发生烷基化反应，此后经过C18柱和CM柱进行分离纯化，得到目标产物。整个过程需时约40 min，最终产品放化收率30%（未经时间校正），放化纯度≥99%，室温下可稳定放置6 h。本方法简便易行，合成时间短，收率较高，产品稳定性好，且其它各项指标均符合规定，为临床常规应用提供了保证。

关键词: ¹⁸F-氟乙基胆碱（¹⁸F-FECH）, 显像剂, PET, 自动化合成

Abstract: ¹⁸F-fluoroethylcholine （¹⁸F-FECH） which reflects the metabolism of choline has been demonstrated to be an promising tumor imaging agent for PET, especially in brain tumor imaging. For utilization in the clinic, this tracer was radiosynthesized automatically with high yields and short synthesis time by using PET-MF-2V-IT-I fluoro-multifunction synthesizer. The two step reactions were processed in the same reaction vessel. The target product was obtained via C18 and CM Sep-pak Plus cartridge with about 30% radiochemical yield (no decay corrected) and more than 99% radiochemical purity within 40 min of total synthesis time, which was stable for 6 h at room temperature. The automatic radiosynthesis procedure have some advantage, such as easy, high yields and short synthesis time and it has potentially utilizable in routine production sites.

Key words: ¹⁸F-fluoroethylcholine （¹⁸F-FECH）, imaging agents, PET, automatic synthesis

党永红;李方;吕京桥;邢海群. PET肿瘤显像剂¹⁸F-氟乙基胆碱的自动化合成[J]. 同位素, 2010, 23(2): 81-85.

DANG Yong-hong; LI Fang; Lü Jing-qiao;XING Hai-qun. Automatic Synthesis of Tumor Imaging Agent ¹⁸F-fluoroethylcholine[J]. Journal of Isotopes, 2010, 23(2): 81-85.

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PET肿瘤显像剂¹⁸F-氟乙基胆碱的自动化合成

Automatic Synthesis of Tumor Imaging Agent ¹⁸F-fluoroethylcholine

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