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Evaluation and improvement of CuI-mediated 11C-cyanation
https://repo.qst.go.jp/records/2000653
https://repo.qst.go.jp/records/200065377e77028-b5d7-480c-977a-3e9495fc4eaa
| アイテムタイプ | 学術雑誌論文 / Journal Article(1) | |||||||||||||||||||||
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| 公開日 | 2024-09-02 | |||||||||||||||||||||
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| タイトル | Evaluation and improvement of CuI-mediated 11C-cyanation | |||||||||||||||||||||
| 言語 | en | |||||||||||||||||||||
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| 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 | |||||||||||||||||||||
| 著者 |
Ishii Hideki
× Ishii Hideki
× Yamasaki Tomoteru
× Okamura Toshimitsu
× Yiding Zhang
× Yusuke Kurihara
× Ogawa Masanao
× Nengaki Nobuki
× Zhang Ming-Rong
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| 抄録 | ||||||||||||||||||||||
| 内容記述タイプ | Abstract | |||||||||||||||||||||
| 内容記述 | CuI-mediated 11C-cyanation was evaluated by synthesizing [11C]perampanel ([11C]5) as a model compound and compared with previous reports. To a DMF solution with 50 -(2-bromophenyl)-10 -phenyl-[2,30 -bipyridin]-60 (10 H)-one (4) and CuI, [11C]NH4CN in a stream of ammonia/nitrogen (5:95, v/v) gas was bubbled. Subsequently, the reaction mixture was heated at 180C for 5 min. After HPLC purification, [11C]5 was obtained in 7.2 ± 1.0% (n = 4) non-decay corrected radiochemical yield with >99% radiochemical purity and a molar activity of 98 ± 28 GBq/μmol. In vivo evaluations of [11C]5 were performed using small animals. PET scans to check the kinetics of [11C]5 in the whole body of mice suggested that [11C]5 spreads rapidly into the brain, heart, and lungs and then accumulates in the small intestine. To evaluate the performance of CuImediated 11C-cyanation reaction, bromobenzene (6a) was selected as the model compound; however, it failed. Therefore, optimization of the reaction conditions has been performed, and consequently, the addition of K2CO3 and prolonging the reaction time improved the radiochemical yield about double. With this improved method, CuI-mediated 11C-cyanation of various (hetero) aromatic bromides was performed to exhibit the tolerance of most functional groups and to provide 11C-cyanated products in good to moderate radiochemical yields. KEYWORDS [11C]ammonium cyanide, [11C]perampanel, carbon-11, copper(I) iodide, positron emission tomography, radiosynthesis |
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| 書誌情報 |
Journal of Labelled Compounds and Radiopharmaceuticals 巻 66, 号 3, p. 95-107, 発行日 2023-05 |
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| 出版者 | Wiley | |||||||||||||||||||||
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| 収録物識別子タイプ | ISSN | |||||||||||||||||||||
| 収録物識別子 | 1099-1344 | |||||||||||||||||||||
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| 識別子タイプ | DOI | |||||||||||||||||||||
| 関連識別子 | 10.1002/jlcr.4016 | |||||||||||||||||||||
