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Novel synthesis of 11C-labelled imidazolines via Pd(0)-mediated 11C-carbomethoxylation using [11C]CO and arylborons
https://repo.qst.go.jp/records/2000860
https://repo.qst.go.jp/records/2000860265e495a-7aea-4fbe-9e3f-cb52f014ef56
| Item type | 学術雑誌論文 / Journal Article(1) | |||||||||||||||
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| 公開日 | 2025-04-11 | |||||||||||||||
| タイトル | ||||||||||||||||
| タイトル | Novel synthesis of 11C-labelled imidazolines via Pd(0)-mediated 11C-carbomethoxylation using [11C]CO and arylborons | |||||||||||||||
| 言語 | en | |||||||||||||||
| 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 | |||||||||||||||
| 著者 |
Ishii Hideki
× Ishii Hideki
× Minegishi Katsuyuki
× Nagatsu Kotaro
× Nengaki Nobuki
× Zhang Ming-Rong
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| 抄録 | ||||||||||||||||
| 内容記述タイプ | Abstract | |||||||||||||||
| 内容記述 | A labeling technique was developed for the imidazoline I2 receptor ligand 2-(3-fluoro-tolyl)-4, 5-dihydro-1H-imidazole (FTIMD) using Pd(0)-mediated 11C-carbomethoxylation with [11C]CO, followed by imidazoline ring formation with ethylenediamine-trimethylaluminium (EDA-AlMe3). To achieve this, [ 11C]CO was passed through a methanol (MeOH) solution containing 3-fluoro4-methylphenylboronic acid (1), palladium (II) acetate (Pd [OAc]2), triphenylphosphine (PPh3), and p-benzoquinone (PBQ). The mixture was then heated at 65!C for 5 min. EDA was introduced into the reaction mixture, and MeOH was completely evaporated at temperatures exceeding 100!C. The dried reaction mixture was combined with an EDA-AlMe (1:1) toluene solution and heated at 145!C for 10 min. Portions of the reaction mixture were analyzed through high-performance liquid chromatography, resulting in [11C]FTIMD with 26% (n = 2) decay-corrected radiochemical yield (RCY). This method could be utilized for various arylborons to produce [2-11C]imidazolines 4a?h with RCYs ranging from low to moderate. Notably, [2-11C]benazoline was obtained with a moderate RCY of 65%. The proposed technique serves as an alternative to the Grignard method, which uses [11C]CO to generate a [2-11C]- labeled imidazoline ring. |
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| 書誌情報 |
Journal of Labelled Compounds and Radiopharmaceuticals 巻 67, 号 6, 発行日 2023-11 |
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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 | |||||||||||||||
| DOI | ||||||||||||||||
| 識別子タイプ | DOI | |||||||||||||||
| 関連識別子 | 10.1002/jlcr.4072 | |||||||||||||||
