Improved automated synthesis of [¹⁸F]fluoroethylcholine as a radiotracer for cancer imaging

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• 作者：M. Piel ; A. Bauman ; R.P. Baum ; S. Hö ; hnemann ; I. Klette ; R. Wortmann ; F. Rö ; sch
• 关键词：[¹⁸F]Fluoroethylcholine ; ¹⁸F-Fluoroalkylation ; Positron emission tomography
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2007
• 期刊代码：9_09680896
• 类别：ch
• 出版时间：1 May 2007
• 卷：15
• 期：9
• 页码：3171-3175
• 文件大小：315 K

摘要

[¹⁸F]Fluoroethylcholine has been recently introduced as a promising ¹⁸F-labelled analogue of [¹¹C]choline which had been previously described as a tracer for metabolic cancer imaging with positron emission tomography (PET). Due to the practical advantages of using the longer-lived radioisotope ¹⁸F (t_1/2 = 110 min), offering the opportunity of a more widespread clinical application, we established a reliable, fully automated synthesis for its production using a modified, commercially available module. [¹⁸F]Fluoroethylcholine was prepared from N,N-dimethylaminoethanol by iodide catalyzed alkylation with 1-[¹⁸F]fluoro-2-tosylethane as alkylating agent, resulting in a total radiochemical yield of 30 ± 6%after a synthesis time of 50 min. The specific activity of [¹⁸F]fluoroethylcholine was >55 GBq/μmol and the radiochemical purity 95–99%.