No-carrier-added electrochemical nucleophilic radiofluorination of aromatics
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Direct nucleophilic radiosynthesis of di-tert-butyl-(4-[18F]fluoro-1,2-phenylene)-dicarbonate was conducted through no-carrier-added electrochemical reactions. 10 mM of triethylamine acetic acid (Et3N·3HAc) in acetonitrile was used to release [18F]fluoride ion trapped in the quaternary ammonium anion exchange resin. The relationship between radiofluorination efficiency, concentration of the Et3N·3HAc, and the working potential were studied with a di-tert-butyl-(4-(tert-butyl)-1,2-phenylene)-dicarbonate substrate in nonaqueous acetonitrile solution. Radiochemical yields of 6.8 ± 1.3 % with specific activity of up to 13 GBq/µmol were achieved with a precursor concentration of 50 mM after a reaction time of 57 min at 0 °C.
KeywordsPET Radiochemistry No-carrier-added radiosynthesis Electrochemical radiosynthesis Nucleophilic fluorination [18F]Fluoride
This project is supported by the START Fellowship program from US Department of Energy. We thank the UCLA Biomedical Cyclotron staff for their help with radioisotope delivery and Mr. P. Marchis and C. Bobinski for their help with radiochemistry setup. We thank Dr. A. Lebedev for the help with development of the automated platform. We thank Dr. E. Nouri-Nigjeh for the assistance of LC–MS measurements.
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