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How to increase the reactivity of [18F]fluoroethyl bromide: [18F]fluoroethylation of amine, phenol and amide functional groups with [18F]FEtBr, [18F]FEtBr/NaI and [18F]FEtOTf
https://repo.qst.go.jp/records/44330
https://repo.qst.go.jp/records/443304150c870-6f74-4f67-be13-10e7499ebeda
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2006-06-23 | |||||
| タイトル | ||||||
| タイトル | How to increase the reactivity of [18F]fluoroethyl bromide: [18F]fluoroethylation of amine, phenol and amide functional groups with [18F]FEtBr, [18F]FEtBr/NaI and [18F]FEtOTf | |||||
| 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 |
Zhang, Ming-Rong
× Zhang, Ming-Rong× Furutsuka, Kenji× Yoshida, Yuichirou× Suzuki, Kazutoshi× 張 明栄× 古塚 賢士× 吉田 勇一郎× 鈴木 和年 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | [18F]Fluoroethyl bromide ([18F]FEtBr) is a useful synthetic precursor to synthesize 18F-labeled compounds. However, the lower reactivity of [18F]FEtBr with amine, phenol and amide functional groups than that of [11C]CH3I partly limits its wide application in the synthesis of [18F]fluoroethylated compounds. The aim of this study was to increase the reactivity of [18F]FEtBr with various nucleophilic substrates for PET tracers containing amine, phenol and amide moieties. The present strategies included (1) adding NaI into the reaction mixture of [18F]FEtBr and substrate, where [18F]FEtI is reversibly formed and becomes more reactive; 2) converting [18F]FEtBr into much more reactive [18F]FEtOTf, similar to conversion of [11C]CH3I into [11C]CH3OTf. By these efforts, the [18F]fluoroethylation efficiency of various substrates containing amine, phenol and amide groups with [18F]FEtBr/NaI and [18F]FEtOTf was significantly improved, compared with the corresponding reaction efficiency with [18F]FEtBr. | |||||
| 書誌情報 |
Journal of Labelled Compounds & Radiopharmaceuticals 巻 46, p. 587-598, 発行日 2003 |
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| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0362-4803 | |||||
