4.8 Article

Synthesis of 18F-difluoromethylarenes using aryl boronic acids, ethyl bromofluoroacetate and [18F]fluoride

Journal

CHEMICAL SCIENCE
Volume 10, Issue 11, Pages 3237-3241

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c8sc05096a

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Funding

  1. Pfizer
  2. Engineering and Physical Sciences Research Council [EP/N509711/1]
  3. Cancer Research UK [C5255/A16466]
  4. Agency for Science, Technology and Research (A*STAR, Singapore)
  5. UCB
  6. EPSRC [1809880] Funding Source: UKRI

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Herein, we report the radiosynthesis of F-18-difluoromethylarenes via the assembly of three components, a boron reagent, ethyl bromofluoroacetate, and cyclotron-produced non-carrier added [F-18] fluoride. The two key steps are a copper-catalysed cross-coupling reaction, and a Mn-mediated F-18-fluorodecarboxylation.

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