有机化学 ›› 2011, Vol. 31 ›› Issue (01): 54-62. 上一篇    下一篇

综述与进展

NH-1,2,3-三唑合成进展

张文生*,1,匡春香*,2,杨青3   

  1. (1焦作师范高等专科学校生化系 焦作 454001)
    (2同济大学化学系 上海 200092)
    (3复旦大学生命科学学院 上海 200433)
  • 收稿日期:2010-04-07 修回日期:2010-05-13 发布日期:2010-06-22
  • 通讯作者: 张文生 E-mail:tongjizws@163.com
  • 基金资助:

    国家自然科学基金;河南省教育厅自然科学研究计划项目

Advances in the Synthesis of NH-1,2,3-Triazoles

Zhang Wensheng*,1 Kuang Chunxiang*,2 Yang Qing3   

  1. (1 Department of Chemistry, Jiaozuo Teachers College, Jiaozuo 454001)
    (2 Department of Chemistry, Tongji University, Shanghai 200092)
    (3 College of Life Science, Fudan University, Shanghai 200433)
  • Received:2010-04-07 Revised:2010-05-13 Published:2010-06-22
  • Contact: ZHANG Wen-Sheng E-mail:tongjizws@163.com

NH-1,2,3-三唑是一类具有重要生理活性的含氮杂环化合物, 是用途广泛的药物中间体. 通过N-烃基化反应, NH-1,2,3-三唑还可以区域选择性的合成各种2-取代-1,2,3-三唑类化合物, 因此是有价值的有机合成中间体. 鉴于NH-1,2,3-三唑在有机合成化学和药物化学中的潜在应用价值, 结合本课题组的研究工作, 对于NH-1,2,3-三唑的主要合成方法, 尤其是近十年来的合成研究进展进行了回顾和展望. 对一些典型的反应机理研究也进行了综述.

关键词: NH-1,2,3-三唑, 合成, 1,3-偶极环加成, 药物中间体

NH-1,2,3-Triazoles are a kind of N-containing heterocylic compounds with important biological activities, which have found broad use in medicinal intermediates. Besides, NH-1,2,3-triazoles serve as valuable synthetic intermediates for the preparation of 2-substituded-1,2,3-triazoles through N-alkylation reaction. Because of their potent applications in both synthetic organic chemistry and medicinal chemistry, the progess in the synthesis of NH-1,2,3-triazoles, especially those reported in the past decade, is surveyed according to the re-search by our group and other groups. Some classical reaction mechanics are also reviewed in this paper.

Key words: NH-1,2,3-triazole, synthesis, 1,3-dipolar cycloaddition, medicinal intermediate