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
Publication date
July 2020
Publisher
American Chemical Society (ACS)
Journal
Organic Letters

Abstract

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

Extracted data

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