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Automated radiosynthesis of two 18F-labeled tracers containing 3-fluoro-2-hydroxypropyl moiety, [18F]FMISO and [18F]PM-PBB3, via [18F]epifluorohydrin
https://repo.qst.go.jp/records/83306
https://repo.qst.go.jp/records/833066fceaa24-bcc1-4c63-931a-6f894dba1891
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2021-06-10 | |||||
| タイトル | ||||||
| タイトル | Automated radiosynthesis of two 18F-labeled tracers containing 3-fluoro-2-hydroxypropyl moiety, [18F]FMISO and [18F]PM-PBB3, via [18F]epifluorohydrin | |||||
| 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 |
Ohkubo, Takayuki
× Ohkubo, Takayuki× Kurihara, Yusuke× Masanao, Ogawa× Nobuki, Nengaki× Masayuki, Fujinaga× Wakana, Mori× Katsushi, Kumata× Masayuki, Hanyu× Kenji, Furutsuka× Hiroki, Hashimoto× Kazunori, Kawamura× Zhang, Ming-Rong× Ohkubo, Takayuki× Kurihara, Yusuke× Masanao, Ogawa× Nobuki, Nengaki× Masayuki, Fujinaga× Wakana, Mori× Katsushi, Kumata× Masayuki, Hanyu× Kenji, Furutsuka× Hiroki, Hashimoto× Kazunori, Kawamura× Zhang, Ming-Rong |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Background [ 18 F]Fluoromisonidazole ([ 18 F]FMISO) and 1-[ 18 F]fluoro-3-((2-((1 E ,3 E )-4-(6-(methylamino)pyridine-3-yl)buta-1,3-dien-1-yl)benzo[d]thiazol-6-yl)oxy)propan-2-ol ([18 F]PM-PBB3 or [ 18 F]APN-1607) are clinically used radiotracers for imaging hypoxia and tau pathology, respectively. Both radiotracers were produced by direct 18 F-fluorination using the corresponding tosylate precursors 1 or 2 and [ 18 F]F - , followed by the removal of protecting groups. In this study, we synthesized [ 18F]FMISO and [ 18 F]PM-PBB3 by 18 F-fluoroalkylation using [ 18 F]epifluorohydrin ([ 18 F] 5 ) for clinical applications. Results First, [ 18 F] 5 was synthesized by the reaction of 1,2-epoxypropyl tosylate ( 8 ) with [ 18 F]F - and was purified by distillation. Subsequently, [ 18 F] 5 was reacted with 2-nitroimidazole ( 6 ) or PBB3 ( 7 ) as a precursor for 18 F-labeling, and each reaction mixture was purified by preparative high-performance liquid chromatography and formulated to obtain the [ 18 F]FMISO or [ 18 F]PM-PBB3 injection. All synthetic sequences were performed using an automated 18 F-labeling synthesizer. The obtained [ 18 F]FMISO showed sufficient radioactivity (0.83 ± 0.20 GBq at the end of synthesis (EOS); n = 8) with appropriate radiochemical yield based on [ 18F]F - (26 ± 7.5% at EOS, decay-corrected; n = 8). The obtained [ 18 F]PM-PBB3 also showed sufficient radioactivity (0.79 ± 0.10 GBq at EOS; n = 11) with appropriate radiochemical yield based on [ 18 F]F - (16 ± 3.2% at EOS, decay-corrected; n = 11). Conclusions Both [ 18 F]FMISO and [ 18 F]PM-PBB3 injections were successfully synthesized with sufficient radioactivity by 18 F-fluoroalkylation using [ 18 F] 5 . |
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| 書誌情報 |
EJNMMI Radiopharmacy and Chemistry 巻 6, p. 23, 発行日 2021-07 |
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| 出版者 | ||||||
| 出版者 | SPRINGER NATURE | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 2365-421X | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1186/s41181-021-00138-9 | |||||
| 関連サイト | ||||||
| 識別子タイプ | URI | |||||
| 関連識別子 | https://ejnmmipharmchem.springeropen.com/articles/10.1186/s41181-021-00138-9 | |||||
