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Comparison between [18F]fluorination and [18F]fluoroethylation reactions for the synthesis of the PDE10A PET radiotracer [18F]MNI-659
https://repo.qst.go.jp/records/48388
https://repo.qst.go.jp/records/48388c9078a03-3143-49b9-a801-7b4470cee672
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2017-11-30 | |||||
| タイトル | ||||||
| タイトル | Comparison between [18F]fluorination and [18F]fluoroethylation reactions for the synthesis of the PDE10A PET radiotracer [18F]MNI-659 | |||||
| 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_6501 | |||||
| 資源タイプ | journal article | |||||
| 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 |
Mori, Wakana
× Mori, Wakana× Takei, Makoto× Furutsuka, Kenji× Fujinaga, Masayuki× Kumata, Katsushi× Muto, Masatoshi× Ohkubo, Takayuki× Hashimoto, Hiroki× Tamagnan, Gilles× Higuchi, Makoto× Kawamura, Kazunori× Zhang, Ming-Rong× 森 若菜× 武井 誠× 古塚 賢士× 藤永 雅之× 熊田 勝志× 武藤 正敏× 大久保 崇之× 橋本 裕輝× 樋口 真人× 河村 和紀× 張 明栄 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Introduction: 2-(2-(3-(4-(2-[18F]Fluoroethoxy)phenyl)-7-methyl-4-oxo-3,4-dihydroquinazolin-2-yl)ethyl)-4-isopropoxyisoindoline-1,3-dione ([18F]MNI-659, [18F]1) is a useful PET radiotracer for imaging phosphodiesterase 10A (PDE10A) in human brain. [18F]1 has been previously prepared by direct [18F]fluorination of a tosylate precursor 2 with [18F]F-. The aim of this study was to determine the conditions for the [18F]fluorination reaction to obtain [18F]1 of high quality and with sufficient radioactivity for clinical use in our institute. Moreover, we synthesized [18F]1 by [18F]fluoroethylation of a phenol precursor 3 with [18F]fluoroethyl bromide ([18F]FEtBr), and the outcomes of [18F]fluorination and [18F]fluoroethylation were compared. Methods: We performed the automated synthesis of [18F]1 by [18F]fluorination and [18F]fluoroethylation using a multi-purpose synthesizer. We determined the amounts of tosylate precursor 2 and potassium carbonate as well as the reaction temperature for direct [18F]fluorination. Results: The efficiency of the [18F]fluorination reaction was strongly affected by the amount of 2 and potassium carbonate. Under the determined reaction conditions, [18F]1 with 0.82 ± 0.2 GBq was obtained in 13.6 ± 3.3 % radiochemical yield (n = 8, decay-corrected to EOB and based on [18F]F-) at EOS, starting from 11.5 ± 0.4 GBq of cyclotron-produced [18F]F-. On the other hand, the [18F]fluoroethylation of 3 with [18F]FEtBr produced [18F]1 with 1.0 ± 0.2 GBq and in 22.5 ± 2.5 % radiochemical yields (n = 7, decay-corrected to EOB and based on [18F]F-) at EOS, starting from 7.4 GBq of cyclotron-produced [18F]F-. Clearly, [18F]fluoroethylation resulted in a higher radiochemical yield of [18F]1 than [18F]fluorination. Conclusion: [18F]1 of high quality and with sufficient radioactivity was successfully radiosynthesized by two methods. [18F]1 synthesized by direct [18F]fluorination has been approved and will be provided for clinical use in our institute. |
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| 書誌情報 |
Nuclear Medicine and Biology 巻 55, p. 12-18, 発行日 2017-10 |
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| 出版者 | ||||||
| 出版者 | Elsevier | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0969-8051 | |||||
| PubMed番号 | ||||||
| 識別子タイプ | PMID | |||||
| 関連識別子 | 28972915 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1016/j.nucmedbio.2017.08.002 | |||||
