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Automated radiosynthesis of 18F-fluoromethylated tracers using the simplified one-pot 18F-fluoromethylation via [18F]fluoromethyl tosylate.
https://repo.qst.go.jp/records/86395
https://repo.qst.go.jp/records/86395cf0c5387-53c8-431c-99ea-6dc493577299
| Item type | 会議発表用資料 / Presentation(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2022-06-28 | |||||
| タイトル | ||||||
| タイトル | Automated radiosynthesis of 18F-fluoromethylated tracers using the simplified one-pot 18F-fluoromethylation via [18F]fluoromethyl tosylate. | |||||
| 言語 | ||||||
| 言語 | eng | |||||
| 資源タイプ | ||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_c94f | |||||
| 資源タイプ | conference object | |||||
| アクセス権 | ||||||
| アクセス権 | metadata only access | |||||
| アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
| 著者 |
Kazunori, Kawamura
× Kazunori, Kawamura× Wakana, Mori× Masayuki, Fujinaga× Kurihara, Yusuke× Masanao, Ogawa× Kaito, Tsukagoe× Ohkubo, Takayuki× Hiroki, Hashimoto× Nobuki, Nengaki× Zhang, Ming-Rong× Kazunori, Kawamura× Wakana, Mori× Masayuki, Fujinaga× Kurihara, Yusuke× Masanao, Ogawa× Kaito, Tsukagoe× Ohkubo, Takayuki× Hiroki, Hashimoto× Nobuki, Nengaki× Zhang, Ming-Rong |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Background/Aims: [18F]Fluoroalkyl groups are essential labeling units because they are considered as surrogates for [11C]methyl moieties, and are coupled to the same functional units as the [11C]methyl group. Many [18F]fluoroalkyated PET tracers have been developed. In general, 18F-fluoroalkylation using [18F]fluoroalkyl reagents requires multi-step radiosynthesis procedures and a multi-pot 18F-labeling synthesizer. To overcome these limitations, a straightforward one-pot method for 18F-fluoroethylation without azeotropic drying of [18F]F- was developed [1]. We have used an improved one-pot 18F-fluoroethylaion method to synthesize 18F-fluoroethylated tracers [2]. In this study, we further modified this one-pot method suitable for 18F-fluoromethylation, and simplified the automated radiosynthesis of two [18F]fluoromethylated tracers using this method. Methods: We synthesized [18F]fluoromethyl tosylate in a mixture of 18F- in K222/K2CO3 acetonitrile solution including 2% water, bis(tosyloxy)methane and cesium carbonate. Without purification of [18F]fluoromethyl tosylate, we directly added a labeling precursor to this mixture for the simplified one-pot 18F-fluoromethylation. Using this procedure equipped to a 18F-labeling synthesizer, [18F]FCho (a PET tracer for imaging tumor) and [18F]FMeNER-D2 (a PET tracer for imaging norepinephrine transporter) were automatically synthesized by the reactions of their corresponding labeling precursors with [18F]fluoromethyl tosylate, respectively. Results: Using the simplified one-pot 18F-fluoromethylation procedure in the automated radiosynthesis, we achieved [18F]FCho and [18F]FMeNER-D2 in approximately 10% of radiochemical yield from 18F- at the end of irradiation (EOI). Radiosynthesis times and radiochemical purities of two 18F-labeled tracers were approximately 60 min after EOI and over 95%, respectively. Conclusions: We have successively synthesized [18F]FCho and [18F]FMeNER-D2 using the simplified one-pot 18F-fluoromethylation method, and achieved automation for all radiosynthesis processes using an 18F-labeling synthesizer. The present method provides a shorter synthesis time and automated procedures with one-pot for the 18F-fluoromethylation strategy. | |||||
| 会議概要（会議名, 開催地, 会期, 主催者等） | ||||||
| 内容記述タイプ | Other | |||||
| 内容記述 | 第13回世界核医学会(13th Congress of the World Federation of Nuclear Medicine and Biology) | |||||
| 発表年月日 | ||||||
| 日付 | 2022-09-07 | |||||
| 日付タイプ | Issued | |||||
