4.7 Article

Regioselective Fluorination of Imidazo[1,2-a]pyridines with Selectfluor in Aqueous Condition

期刊

JOURNAL OF ORGANIC CHEMISTRY
卷 80, 期 22, 页码 11559-11565

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AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.5b01961

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资金

  1. National Natural Science Foundation of China [21272117, 21502097]
  2. Natural Science Foundation of the Education Department of Jiangsu province [15KJB150015]
  3. Priority Academic Program Development of Jiangsu Higher Education Institutions

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A regioselective synthesis of 3-fluorinated imidazo[1,2-a]pyridines using 1-chloromethyl-4-fluoro-1,4-di-azoinabi cyclo [2.2.2] octane bis (tetrafluoroborate) (Selectfluor) as the fluorinating reagent in aqueous condition is described. In the presence of DMAP, the reaction mainly gave monofluorinated product via electrophilic fluorinated process in moderate to good yields.

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