Fully automated synthesis of b;¹⁸F]fluoromisonidazole using a conventional b;¹⁸F]FDG module

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• 作者：Seung Jun Oh ; Dae Yoon Chi ; Christoph Mosdzianowski ; Jung Young Kim ; Hee Seop Gil ; Se Hun Kang ; Jin Sook Ryu and Dae Hyuk Moon
• 关键词：b ; ¹⁸F&#x5d ; FMISO ; Automated synthesis system ; Tumor hypoxia ; PET imaging ; b ; ¹⁸F&#x5d ; fluoride
• 刊名：Nuclear Medicine and Biology
• 出版年：2005
• 期刊代码：43_09698051
• 类别：ph
• 出版时间：2005
• 卷：32
• 期：8
• 页码：899-905
• 文件大小：224 K

摘要

We developed a new fully automated method for the synthesis of b;¹⁸F]fluoromisonidazole (b;¹⁸F]FMISO) by modifying a commercial FDG synthesizer and its disposable fluid pathway. A three-step procedure was used to prepare the tosylate precursor, 1-(2′-nitro-1′-imidazolyl)-2-O-tetrahydrofuranyl-3-O-toluenesulfonylpropanediol. Using glycerol as the starting material, the precursor was synthesized with a yield of 21%. The optimal labeling conditions for the automated synthesis of b;¹⁸F]FMISO was 10 mg of precursor in acetonitrile (2 ml heated at 105°C for 360 s, followed by heating at 75°C for 280 s and hydrolysis with 1 N HCl at 105°C for 300 s. Using 3.7 GBq of b;¹⁸F]F⁻ as a starting activity, b;¹⁸F]FMISO was obtained with high end-of-synthesis (EOS) radiochemical yields of 58.5±3.5%for 60.0±5.2 min with high-performance liquid chromatography (HPLC) purification. When solid-phase purification steps were added, the EOS radiochemical yields were 54.5±2.8%(337±25 GBq/bc;mol) for 70.0±3.8 min (n