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Synthesis of 18F-Labeled Aryl Fluorosulfates via Nucleophilic Radiofluorination.

Young-Do KwonMin Ho JeonNam Kyu ParkJeong Kon SeoJeongmin SonYoung Hoon RyuSung You HongJoong-Hyun Chun
Published in: Organic letters (2020)
Sulfuryl fluoride gas is a key reagent for SO2F transfer. However, conventional SO2F transfer reactions have limited 18F-radiochemistry translation, due to the inaccessibility of gaseous [18F]SO2F2. Herein, we report the first SO2F2-free synthesis of aryl [18F]fluorosulfates from both phenolic and isolated aryl imidazylate precursors with cyclotron-produced 18F-. 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 [18F]fluorosulfate.
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