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Synthesis of (R,S)-[4-11C]baclofen via Michael addition of nitromethane labeled with short-lived 11C
https://repo.qst.go.jp/records/45660
https://repo.qst.go.jp/records/4566044245a01-4d09-4f9b-be12-bf42e77eb8a1
Item type | 学術雑誌論文 / Journal Article(1) | |||||
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公開日 | 2009-10-15 | |||||
タイトル | ||||||
タイトル | Synthesis of (R,S)-[4-11C]baclofen via Michael addition of nitromethane labeled with short-lived 11C | |||||
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 |
Kato, Koichi
× Kato, Koichi× Zhang, Ming-Rong× Suzuki, Kazutoshi× 加藤 孝一× 張 明栄× 鈴木 和年 |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | The synthesis of (R,S)-[4-11C]baclofen, the first 11C-labeled GABAB agonist, was demonstrated via Michael addition of nitro[11C]methane as a key step. A tetrabutylammonium fluoride promoted Michael addition of nitro[11C]methane to methyl p-chlorocinnamate, followed by the nitro-group reduction in the presence of NiCl2 and NaBH4 in aqueous MeOH and alkaline hydrolysis yielded (R,S)-[4-11C]baclofen in 36.4+/-1.8% radiochemical conversion in three steps within 20 min. | |||||
書誌情報 |
Bioorganic & Medicinal Chemistry Letters 巻 19, 号 21, p. 6222-6224, 発行日 2009-11 |
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ISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 0960-894X |