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文章基本信息

  • 标题:Microflow Fluorinations of Benzynes: Efficient Synthesis of Fluoroaromatic Compounds
  • 作者:Takashi Ikawa ; Shigeaki Masuda ; Shuji Akai
  • 期刊名称:Chemical and Pharmaceutical Bulletin
  • 印刷版ISSN:0009-2363
  • 电子版ISSN:1347-5223
  • 出版年度:2018
  • 卷号:66
  • 期号:12
  • 页码:1153-1164
  • DOI:10.1248/cpb.c18-00578
  • 语种:English
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:Fluorinated aromatic compounds are found in a variety of biologically active compounds, including clinical drugs and agrochemicals. Therefore, the synthesis of aryl fluorides is particularly important in the medicinal and process chemistry fields. In this paper, we report a method for the synthesis of aryl fluorides by benzyne fluorination under microflow conditions using the efficient Comet X-01 micromixer. In comparison to our previously reported method under ordinary batch conditions, this approach facilitates a significant reduction in reaction times, to ca. 10 s, as well as increases in the yields of fluoroarenes (by up to 51%).
  • 关键词:benzyne;microflow reaction;aromatic fluorination;nonafluorobutanesulfonate;silyl group;tetrabutylammonium fluoride
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