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Synthesis of 11C-labeled retinoic acid, [11C]ATRA, via an alkenylboron precursor by Pd(0)-mediated rapid C-[11C]methylation
https://repo.qst.go.jp/records/46819
https://repo.qst.go.jp/records/4681984f5783b-813a-4501-b587-ec333de257af
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2014-09-01 | |||||
| タイトル | ||||||
| タイトル | Synthesis of 11C-labeled retinoic acid, [11C]ATRA, via an alkenylboron precursor by Pd(0)-mediated rapid C-[11C]methylation | |||||
| 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 |
Suzuki, Masaaki
× Suzuki, Masaaki× Takashima-Hirano, Misato× Ishii, Hideki× Watanabe, Chika× Sumi, Kengo× Koyama, Hiroko× Doi, Hisashi× 石井 英樹× 土居 久志 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Retinoids are a class of chemical compounds which include both natural dietary vitamin A (retinol) metabolites and active synthetic analogs. Both experimental and clinical studies have revealed that retinoids regulate a wide variety of essential biological processes. In this study, we synthesized 11C-labeled all-trans-retinoic acid (ATRA), the most potent biologically active metabolite of retinol and used in the treatment of acute promyelocytic leukemia. The synthesis of 11C-labeled ATRA was accomplished by a combination of rapid Pd(0)-mediated C-[11C]methylation of the corresponding pinacol borate precursor prepared by 8 steps and hydrolysis. [11C]ATRA will prove useful as a PET imaging agent, particularly for elucidating the improved therapeutic activity of ATRA (natural retinoid) for acute promyelocytic leukemia by comparing with the corresponding PET probe [11C]Tamibarotene (artificial retinoid). |
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| 書誌情報 |
Bioorganic & Medicinal Chemistry Letters 巻 24, 号 15, p. 3622-3625, 発行日 2014-08 |
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| 出版者 | ||||||
| 出版者 | Elsevier | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | DOI:10.1016/j.bmcl.2014.05.04/ | |||||
