Synthesis of gem-difluorinated 1,6-naphthyridin-5,7-diones

Karel Piron, Sara Kenis, Guido Verniest, Riccardo Surmont, Jan Willem Thuring, Peter Ten Holte, Frederik Deroose, Norbert De Kimpe

Research output: Contribution to journalArticlepeer-review

11 Citations (Scopus)


A synthetic route toward new 8,8-difluoro-1,6-naphthyridine-5,7-diones, which are of interest as new building blocks in pharmaceutical chemistry, is described. The key steps include a copper-mediated cross-coupling of ethyl bromodifluoroacetate and 2-bromo-3-cyanopyridine, followed by hydrolysis of the nitrile function and subsequent cyclization.
Original languageEnglish
Pages (from-to)6941-6947
Number of pages7
Publication statusPublished - 26 Aug 2012


  • organofluorine chemistry
  • heterocycles


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