Synthesis of 18F-Labeled Aryl Fluorosulfates via Nucleophilic Radiofluorination
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- Synthesis of 18F-Labeled Aryl Fluorosulfates via Nucleophilic Radiofluorination
- Kwon, Young-Do; Jeon, Min Ho; Park, Nam Kyu; Seo, Jeong Kon; Son, Jeongmin; Ryu, Young Hoon; Hong, Sung You; Chun, Joong-Hyun
- Issue Date
- AMER CHEMICAL SOC
- ORGANIC LETTERS, v.22, no.14, pp.5511 - 5516
- Sulfuryl fluoride gas is a key reagent for SO2F transfer. However, conventional SO2F transfer reactions have limited F-18-radiochemistry translation, due to the inaccessibility of gaseous [F-18] SO2F2. Herein, we report the first SO2F2-free synthesis of aryl [F-18]fluorosulfates from both phenolic and isolated aryl imidazylate precursors with cyclotron-produced F-18(-) . The radiochemical yields ranged from moderate to good with excellent functional group tolerance. The reliability of our approach was validated by the automated radiosynthesis of 4-acetamidophenyl [F-18]fluorosulfate.
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