研究论文

苯并磺内酰胺联吡唑化合物的简便合成

  • 雷容超 ,
  • 兰文捷 ,
  • 李梦竹 ,
  • 傅滨
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  • 中国农业大学理学院 北京 100193

收稿日期: 2022-09-09

  修回日期: 2022-12-14

  网络出版日期: 2023-02-07

基金资助

国家重点研发计划(2017YFD0200301)

A Convenient Approach to Benzosultam-Linked Pyrazole Compounds

  • Rongchao Lei ,
  • Wenjie Lan ,
  • Mengzhu Li ,
  • Bin Fu
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  • College of Science, China Agricultural University, Beijing 100193

Received date: 2022-09-09

  Revised date: 2022-12-14

  Online published: 2023-02-07

Supported by

National Key Research and Development Program of China(2017YFD0200301)

摘要

报道了一种碱调节的快速合成苯并磺内酰胺联吡唑化合物的方法. 在三乙胺和乙酸酐存在下, 苯并磺内酰亚胺与吡唑-5-酮能够顺利地进行Mannich反应, 并以高收率得到加成产物. 推测了可能的反应机理, 反应放大到克级规模, 同样能够以高收率获得产物.

本文引用格式

雷容超 , 兰文捷 , 李梦竹 , 傅滨 . 苯并磺内酰胺联吡唑化合物的简便合成[J]. 有机化学, 2023 , 43(7) : 2553 -2560 . DOI: 10.6023/cjoc202209009

Abstract

A base-mediated rapid synthesis of benzosultam-linked pyrazole compounds was developed. The reaction of N-sulfonyl ketimine with pyrazolin-5-one proceeded smoothly to provide the desired products in high yields in the presence of Et3N and Ac2O. The possible mechanism was proposed. This reaction could be conducted on a gram-scale with maintained high yield.

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