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アイテム
Automated Synthesis of (rac)‐, (R)‐, and (S)‐[18F]Epifluorohydrin and Their Application for Developing PET Radiotracers Containing a 3‐[18F]Fluoro‐2‐hydroxypropyl Moiety
https://repo.qst.go.jp/records/49146
https://repo.qst.go.jp/records/49146c526c20b-375d-445f-8610-d8563dd7c5d4
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2018-08-03 | |||||
| タイトル | ||||||
| タイトル | Automated Synthesis of (rac)‐, (R)‐, and (S)‐[18F]Epifluorohydrin and Their Application for Developing PET Radiotracers Containing a 3‐[18F]Fluoro‐2‐hydroxypropyl Moiety | |||||
| 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 |
Fujinaga, Masayuki
× Fujinaga, Masayuki× Ohkubo, Takayuki× Yamasaki, Tomoteru× Zhang, Yiding× Mori, Wakana× Hanyu, Masayuki× Kumata, Katsushi× Hatori, Akiko× Xie, Lin× Nengaki, Nobuki× Ming-Rong, Zhang× Fujinaga, Masayuki× Ohkubo, Takayuki× Yamasaki, Tomoteru× Zhang, Yiding× Mori, Wakana× Hanyu, Masayuki× Kumata, Katsushi× Hatori, Akiko× Xie, Lin× Nengaki, Nobuki× Ming-Rong, Zhang |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | To introduce the 3‐[18F]fluoro‐2‐hydroxypropyl moiety into positron emission tomography (PET) radiotracers, we performed automated synthesis of (rac)‐, (R)‐, and (S)‐[18F]epifluorohydrin ([18F]1) by nucleophilic displacement of (rac)‐, (R)‐, or (S)‐glycidyl tosylate with 18F− and purification by distillation. The ring‐opening reaction of (R)‐ or (S)‐[18F]1 with phenol precursors gave enantioenriched [18F]fluoroalkylated products without racemisation. We then synthesised (rac)‐, (R)‐, and (S)‐ 2‐{5‐[4‐(3‐[18F]fluoro‐2‐hydroxypropoxy)phenyl]‐2‐oxobenzo[d]oxazol‐3(2H)‐yl}‐N‐methyl‐N‐phenylacetamide ([18F]6) as novel radiotracers for the PET imaging of translocator protein (18 kDa) and showed that (R)‐ and (S)‐[18F]6 had different radioactivity uptake in mouse bone and liver. Thus, (rac)‐, (R)‐, and (S)‐[18F]1 are effective radiolabelling reagents and can be used to develop PET radiotracers by examining the effects of chirality on their in vitro binding affinities and in vivo behaviour. | |||||
| 書誌情報 |
ChemMedChem 巻 13, p. 1723-1731, 発行日 2018-07 |
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| 出版者 | ||||||
| 出版者 | Wiley | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 1860-7179 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1002/cmdc.201800359 | |||||
