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Radiosynthesis of [18F]FEDAC with the hydrous 18F-fluorination using Kryptofix 222 and potassium carbonate
https://repo.qst.go.jp/records/76116
https://repo.qst.go.jp/records/7611675ebabc3-ab3d-45c4-b627-9b237c703f96
| Item type | 会議発表用資料 / Presentation(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2019-06-03 | |||||
| タイトル | ||||||
| タイトル | Radiosynthesis of [18F]FEDAC with the hydrous 18F-fluorination using Kryptofix 222 and potassium carbonate | |||||
| 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 |
Kawamura, Kazunori
× Kawamura, Kazunori× Kumata, Katsushi× Mori, Wakana× Fujinaga, Masayuki× Kurihara, Yusuke× Ogawa, Masanao× Nengaki, Nobuki× Ming-Rong, Zhang× Kawamura, Kazunori× Kumata, Katsushi× Mori, Wakana× Fujinaga, Masayuki× Kurihara, Yusuke× Ogawa, Masanao× Nengaki, Nobuki× Ming-Rong, Zhang |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Objectives: Most 18F-labeled radiopharmaceuticals are prepared via aliphatic and aromatic nucleophilic substitution reaction with 18F-. Owing to hydration, water significantly diminishes the nucleophilicity of 18F-. To remove the bulk of water, 18F- is trapped on the Sep-Pak QMA cartridge, and water is removed by time-consuming repetitive azeotropic drying from an aqueous solution of potassium carbonate (K2CO3) and Kryptofix 222 (K222) as an elution from the Sep-Pak QMA cartridge. To develop an easy and fast 18F-flurorination without the use of azeotropic drying, Kniess T. et al. established the concept of hydrous 18F-fluorination using K2CO3 and K222 [ref. 1]. Recently, to transfer the production technique of [18F]FEDAC to other PET centers, we developed an efficiently radiosynthetic method of [18F]FEDAC in the one-pot [ref. 2]. To achieve an easy and fast radiosynthesis, we examined the radiosynthesis of [18F]FEDAC with the hydrous 18F-fluorination using K2CO3 and K222 in the one-pot. Methods: [18F]FEDAC was synthesized with the hydrous 18F-fluorination in two routes from tosyl-precursor or desmethyl-precursor. [18F]F- was trapped on the Sep-Pak QMA cartridge, and eluted with the solution (1 mL, 0.2% water in acetonitrile) of K222 (12-15 μmol) and K2CO3 (6-8 μmol). In the case of direct 18F-fluorination of tosyl-precursor, the eluent from the Sep-Pak QMA cartridge was loaded into the vessel in which tosyl-precursor (1-4 mg, 3-7 μmol) was added in advance, and the mixture solution was heated at 100ºC for 15 min. After the solution was evaporated to dryness, the eluent of HPLC was added into the vessel and the reaction mixture was loaded into the injector of preparative HPLC. In the case of 18F-fluoroethylation of desmethyl-precurosor in the one-pot, the eluent from the Sep-Pak QMA cartridge was loaded into the vessel in which ethylene glycol ditosylate (2.4-3.1 mg, 7-8 μmol) and cesium carbonate (2.1-2.8 mg, 7-8 μmol) were added in advance, and the mixture solution was heated at 100ºC for 5 min. After the solution was evaporated to dryness, the desmethyl-precursor (2.6-3.0 mg, 7-8 μmol) in DMSO (0.5 mL) was added into the vessel and the mixture solution was heated at 100ºC for 15 min. After the eluent of HPLC was added into the vessel, the reaction mixture was loaded into the injector of preparative HPLC. HPLC fractions of [18F]FEDAC were collected and evaporated to dryness, and the residue was dissolved in physiological saline. Results: In the radiosynthesis with the hydrous 18F-fluorination of tosylated-precursor, the radiochemical yields (RCYs) from [18F]F- was 15% (1 mg of precursor) at the end of irradiation (EOI). In the previous study with azeotropic drying, the RCY from [18F]F- was 19% (1 mg of precursor) at EOI [ref. 2]. Although the RCY in this study was close to that in the previous study, the present synthesis time (approx. 53 min) was shorter than that in previous study (70 min) [ref. 2]. Furthermore, we optimized this radiosynthesis with the hydrous 18F-fluorination of tosylated-precursor, and the RCY from [18F]F- was achieved over 20% at EOI by the use of 4 mg (7 μmol) of precursor. In the case of 18F-fluoroethylation of desmethyl-precursor in the one-pot, the RCY from [18F]F- was approximately 10% at EOI. In the previous study with azeotropic drying in the two-pots, the RCY from [18F]F- was 24% (1 mg of precursor) at EOI [ref. 2]. Although the RCY in this study was lower than that in the two-step reaction, the present synthesis time (60 min) was shorter than that in previous study (90 min). Conclusion: We enabled to synthesize [18F]FEDAC easily and rapidly with the hydrous 18F-fluorinaiton in the one-pot. References: [1] T. Kniess, M. Laube, and J, Steinbach, Appl Radiat Isot. 2017, 127, 260–8. [2] K. Kawamura, K. Kumata. T. Takei. et al, Nucl Med Biol. 2016, 43, 445–53. |
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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 | ISRS2019 | |||||
| 発表年月日 | ||||||
| 日付 | 2019-05-27 | |||||
| 日付タイプ | Issued | |||||
