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Asymmetric Synthesis of Chiral Sulfoximines via the 5-Arylation of Sulfinamides

机译:通过亚磺酰胺的5-丙烯酸酯化反应不对称合成手性亚砜肟

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摘要

Optically active sulfoximines are a promising substance in medicinal chemistry. However, a methodology for preparing chiral sulfoximines in a stereoselective manner has been underdeveloped. Here, we report an asymmetric synthesis of chiral sulfoximines having an aryl group by the newly developed sulfur-selective arylation of easily accessible chiral sulfinamides. The utility of the present method is demonstrated by the asymmetric synthesis of a key intermediate of a COX-2 inhibitor.
机译:光学活性磺胺嘧啶在药物化学中是很有前途的物质。然而,以立体选择性方式制备手性亚砜亚胺的方法尚未得到开发。在这里,我们通过易于开发的手性亚磺酰胺的硫磺选择性芳基化反应,报道了具有芳基的手性亚砜肟的不对称合成。通过COX-2抑制剂关键中间体的不对称合成证明了本方法的实用性。

著录项

  • 来源
    《Journal of the American Chemical Society》 |2019年第49期|19263-19268|共6页
  • 作者单位

    Department of Chemistry Graduate School of Science Kyoto University;

    Department of Chemistry Graduate School of Science Kyoto University|Laboratory of Organocatalyst Chemistry Graduate School of Pharmaceutical Sciences Kyoto University|School of Chemical Engineering and Light Industry Guangdong University of Technology;

  • 收录信息 美国《科学引文索引》(SCI);美国《工程索引》(EI);美国《生物学医学文摘》(MEDLINE);美国《化学文摘》(CA);
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类
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  • 入库时间 2022-08-18 04:58:35

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