Результаты исследований: Научные публикации в периодических изданиях › статья › Рецензирование
Radiofluorination of arylboronic acids pinacol esters (arylBPin) mediated by copper triflate pyridine complex is one of the more promising synthetic approaches for the direct introduction of nucleophilic [18F]fluoride into non-activated arenes and heteroarenes. However, the application of this method to the production of positron emission tomography (PET) radiotracers in automated synthesizers remains a challenging task. The choice of phase-transfer catalyst (PTC) and corresponding base used for the generation of reactive [18F]fluoride species has a profound impact on the efficiency of the 18F-fluorination process. Herein we report the development of a simple procedure involving trapping of the aqueous [18F]fluoride on a weak anion-exchange resin (WAX) and its release by elution with pyridinium sulfonate in dimethyl acetamide. Obtained reactive [18F]fluoride was used as-is in a copper-catalyzed fluorination reaction employing pyridinium salt as both PTC and base. High radiochemical conversion rates (RCCs) achieved for a series of simple arylBPin substrates and 4-[18F]fluoro-D,L-phenylalanine demonstrate the efficiency of this novel 18F-processing approach. Notably, the proposed method obviates conventional azeotropic drying steps, solvents evaporation and/or changeover and can be implemented on commercial automated synthesizers.
| Язык оригинала | английский |
|---|---|
| Страницы (с-по) | 918-922 |
| Число страниц | 5 |
| Журнал | European Journal of Organic Chemistry |
| Том | 2019 |
| Номер выпуска | 5 |
| DOI | |
| Состояние | Опубликовано - 7 фев 2019 |
ID: 38812255