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Pd(0)-mediated [11C]carbonylation of boronic acid pinacol esters with [11C]carbon monoxide and the facile conversion of [carbonyl-11C]esters to [carbonyl-11C]amides
https://repo.qst.go.jp/records/65681
https://repo.qst.go.jp/records/656818321f604-a8f9-4294-adc5-81641e3eaf6d
| Item type | 会議発表用資料 / Presentation(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2015-06-17 | |||||
| タイトル | ||||||
| タイトル | Pd(0)-mediated [11C]carbonylation of boronic acid pinacol esters with [11C]carbon monoxide and the facile conversion of [carbonyl-11C]esters to [carbonyl-11C]amides | |||||
| 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_c94f | |||||
| 資源タイプ | conference object | |||||
| 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 |
Ishii, Hideki
× Ishii, Hideki× Minegishi, Katsuyuki× Nagatsu, Koutarou× Zhang, Ming-Rong× 石井 英樹× 峯岸 克行× 永津 弘太郎× 張 明栄 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Objectives: Introduction of carbonyl moiety into an aryl or heteroaryl group are powerful processes for the construction of valuable pharmacophore. However typical carbonylation reaction using [11C]O generally requires high pressure and high temperature conditions. Therefore, the development of convenient method for the [11C]carbonylation reaction is needed. Here we present the Pd(0)-mediated mild [11C]carbonylation reaction using [11C]O and boronic acid pinacol esters. Methods: The [11C]O, which prepared from [11C]O2, was reacted with aryl and heteroarylboronic acid pinacol esters in the presence of p-benzoquinone and triphenylphosphine in MeOH or DMF-MeOH (v/v =1:1) at 65 °C under atmospheric pressure for 5 min to give corresponding [11C]esters. Some of these [11C]esters were converted to corresponding [11C]amides by treatment with 25% ammonia solution 65 °C for 5 min. Scheme 1. Radiosynthesis of [carbonyl-11C]esters and [carbonyl-11C]amides \nResults: Various aryl/heteroaryl boronates were converted to the corresponding [carbonyl-11C]esters with decay-corrected radiochemical yield in the range of 6-80% Conclusions: Acknowledgeme |
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| 会議概要（会議名, 開催地, 会期, 主催者等） | ||||||
| 内容記述タイプ | Other | |||||
| 内容記述 | 21st International Symposium on Radiopharmaceutical Sciences | |||||
| 発表年月日 | ||||||
| 日付 | 2015-05-29 | |||||
| 日付タイプ | Issued | |||||
