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SNAr Radiofluorination with In Situ Generated [18F]Tetramethylammonium Fluoride.

So Jeong LeeMaría T Morales-ColónAllen F BrooksJay S WrightKatarina J MakaravagePeter J H ScottMelanie S Sanford
Published in: The Journal of organic chemistry (2021)
This report describes a method for the nucleophilic radiofluorination of (hetero)aryl chlorides, (hetero)aryl triflates, and nitroarenes using a combination of [18F]KF·K2.2.2 and Me4NHCO3 for the in situ formation of a strongly nucleophilic fluorinating reagent (proposed to be [18F]Me4NF). This method is applied to 24 substrates bearing diverse functional groups, and it generates [18F](hetero)aryl fluoride products in good to excellent radiochemical yields in the presence of ambient air/moisture. The reaction is applied to the preparation of 18F-labeled HQ-415 for potential (pre)clinical use.
Keyphrases
  • drinking water
  • air pollution
  • signaling pathway
  • particulate matter
  • lps induced
  • oxidative stress
  • pi k akt
  • pet imaging
  • cell proliferation
  • high resolution