4.8 Article

Catalytic Decarboxylative Fluorination for the Synthesis of Tri- and Difluoromethyl Arenes

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ORGANIC LETTERS
卷 15, 期 11, 页码 2648-2651

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AMER CHEMICAL SOC
DOI: 10.1021/ol4009377

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资金

  1. EU [PIIF-GA-20100274903]
  2. BBSRC
  3. GE Healthcare
  4. EPSRC
  5. Astra-Zeneca
  6. Imanova, the CRUK
  7. Academy of Finland
  8. Finnish Centre of Excellence in Molecular Imaging in Cardiovascular and Metabolic Research
  9. Biotechnology and Biological Sciences Research Council [1112421] Funding Source: researchfish

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Treatment of readily available alpha,alpha-difluoro- and alpha-fluoroarylacetic acids with Selecffluor under Ag(I) catalysis led to decarboxylative fluorination. This operationally simple reaction gave access to tri- and difluoromethylarenes applying a late-stage fluorination strategy. Translation to [F-18]labeling is demonstrated using [F-18]Selectfluor bis(triflate), a reagent affording [F-18]tri- and [F-18]difluoromethylarenes not within reach with [F-18]F-2.

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