ol0c01868_si_001.pdf (13.83 MB)
Synthesis of 18F‑Labeled Aryl Fluorosulfates via Nucleophilic Radiofluorination
journal contribution
posted on 2020-06-26, 14:34 authored by Young-Do Kwon, Min Ho Jeon, Nam Kyu Park, Jeong Kon Seo, Jeongmin Son, Young Hoon Ryu, Sung You Hong, Joong-Hyun ChunSulfuryl 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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Keywords
ArylNucleophilic Radiofluorination Sulfuryl fluoride gasradiochemical yields2 F 2Fluorosulfatesynthesiscyclotron-producedinaccessibility18 F-radiochemistry translation2 F transfer reactionsphenolicradiosynthesi2 F transferapproachgroup tolerancereagent4- acetamidophenylHereinaryl imidazylate precursorsreliabilitySynthesi
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