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  • 标题:Boron-Catalyzed Carboxylic Acid-Selective Aldol Reaction with Trifluoromethyl Ketones
  • 本地全文:下载
  • 作者:Kouhei Ishizawa ; Hideoki Nagai ; Yohei Shimizu
  • 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:3
  • 页码:231-234
  • DOI:10.1248/cpb.c17-00545
  • 语种:English
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:

    A catalytic carboxylic acid-selective aldol reaction with trifluoromethyl ketones was developed. Reversible and selective covalent bond formation between a boron catalyst and a carboxylic acid is key to realizing the unprecedented catalytic aldol reaction of simple carboxylic acids. The reaction proceeded chemoselectively at the α-position of carboxylic acid even in the presence of ketone, ester, or amide functional groups in the donor substrates. The chemoselectivity is beneficial for late-stage derivatizations of biologically relevant compounds, as demonstrated by the conversion of indomethacin and triacetylcholic acid.

  • 关键词:carboxylic acid;aldol reaction;boron catalyst;trifluoromethyl ketone
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