高等学校化学学报 ›› 1995, Vol. 16 ›› Issue (4): 563.

• 论文 • 上一篇    下一篇

1,2,4-三嗪类化合物研究(XXIV)──吡唑并-(5,4-e)-1,2,4-三嗪衍生物的合成

沙耀武, 蔡孟深   

  1. 北京医科大学药学院, 北京, 100083
  • 收稿日期:1994-04-10 修回日期:1994-11-10 出版日期:1995-04-24 发布日期:1995-04-24
  • 通讯作者: 蔡孟深
  • 作者简介:沙耀武,男,32岁,博士研究生.
  • 基金资助:

    国家自然科学基金

Chemistry of 1,2,4-Triazines (XXIV)──Synthesis of Pyrazolo-(5,4-e)-1,2,4-triazine Derivatives

SHA Yao-Wu, CAI Meng-Shen   

  1. School of Pharmaceutical Sciences, Beijing Medical University, Beijing, 100083
  • Received:1994-04-10 Revised:1994-11-10 Online:1995-04-24 Published:1995-04-24

摘要: 先合成1,2,4-三嗪环,然后并接吡唑环,对标题化合物进行了合成研究。对1,2,4-三嗪环上的硫化反应进行了改进,解决了3个反应活性相近部位的选择性肼解问题;并发现了肼基与乙酸乙酯于室温下反应生成1,3,4-二唑环的新反应。

关键词: 吡唑并-(5, 4-e)-1, 2, 4-三嗪, 1, 3, 4-二唑, 1, 2, 4-三嗪

Abstract: Two potential anti-tumour compounds,3-methylthio-7-oxo-7,7,8,9-tetrahy-dropyrazolo-(5,4-e)-1,2,4-triazine(9)and 3-methylthio-7-thio-7,7,8,9-tetrahydropyrazolo(5,4-e)-1,2,4-triazine(10)were synthesized.Anew mild condition was introduced to the thionation of 1,2,4-triazine ring. Selective hyrazinolysis of three positions of similar reactivity on 1,2,4-triazine ring was improved. Anew reaction was applied in the preparation of 1, 3,4-oxa-diazole compound from hydrazyl derivatives with ethyl acetate.

Key words: Pyrazolo-(5,4-e)-1,2,4-triazine, 1,3,4-Oxa-diazole, 1,2,4-Triazine

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