高等学校化学学报

高等学校化学学报 ›› 1994, Vol. 15 ›› Issue (12): 1787.

• 论文 • 上一篇    下一篇

稠杂环化合物的研究(ⅩⅤⅠ)─1－芳基－1,2,3－连三唑[4,5－e]嘧啶酮及哌啶/氢化吖辛因[1,2－b]嘧啶酮类化合物的合成

张自义1, 刘莹1, 陈茂齐2, 杨世琰2   

  1. 1. 兰州大学化学系, 兰州, 730000;
    2. 中国科学院兰州化学物理研究所
  • 收稿日期:1993-12-14 修回日期:1994-06-20 出版日期:1994-12-24 发布日期:1994-12-24
  • 通讯作者: 张自义,男,60岁,教授.
  • 作者简介:张自义,男,60岁,教授.
  • 基金资助:

    国家自然科学基金

Studies on Condensed Heterocyclic Compounds (XVI)─Synthesis of 1-Aryl-1, 2, 3-triazolo[4,5-e] pyrimidineone and Piperidine or Azacyclooctane [1,2-b] pyrimidineone Compounds

ZHANG Zi-Yi1, LIU Ying1, CHEN Mao-Qi2, YANG Shi-Yan2   

  1. 1. Department of Chemistry, Lanzhou University, National Laboratory of Applied Organic Chemistry, Lanzhou, 730000;
    2. Lanzhou Institute of Chemical Physics, Academia Sinica, Lanzhou
  • Received:1993-12-14 Revised:1994-06-20 Online:1994-12-24 Published:1994-12-24

PDF (PC)

摘要： 研究了1-芳基-4-乙氧羰基-5-氨基-1,2,3-连三唑(1)同甲酰胺、异氰酸磺酰氯以及内酰亚胺醚等的反应,制得5-H-1-芳基-1,2,3-连三唑[4,5-e]嘧啶-4-酮(2a-c)、5-N-甲基-1-芳基-1,2,3-连三唑[4,5-e]嘧啶-4-酮(3a-c)、1-芳基-4-乙氧羰基-5-脲基-1,2,3-连三唑(4a,b)、5-H-1-芳基-1,2,3-连三唑[4,5-e]嘧啶-4,6-二酮(5_(a,b))、1-苯基-1,2,3-连三唑[4,5-e]哌啶[1,2-b]嘧啶-4-酮(6a)、1-苯基-1,2,3-连三唑[4,5-e]氢化吖辛因[1,2-b]嘧啶-4-酮(7a),并经元素分析、红外、核磁共振以及质谱等方法确认了它们的结构,初步筛选了其代表特的生物活性。

关键词: 稠杂环, 芳基连三唑并嘧啶酮, 芳基连三唑并哌啶嘧啶酮, 连三唑氢化吖辛因嘧啶酮, 生物活性

Abstract: For the purpose of studying the relationship between molecular structures and biological activies of condensed heterocyclic compounds as a part of our recent progress, a series of new heterocyclic derivatives, 5H-1-aryl-1, 2, 3-triazolo[4, 5-e] pyrimidine-4-one(2a-c), 5-N-methyl-1-aryl-1, 2, 3-triazolo[4, 5-e]pyrimidine-4-one(3a-c), 1-aryl-4-ethoxycarbonyl-5-uramine-1, 2, 3-triazole(4(a, b)), 5H-1-aryl-1, 2, 3-triazolo[4, 5-e] pyrimidine-4, 6-dione( 5(a, b)), 1-aryl-1, 2, 3-triazolo[4, 5-e]piperidine[1, 2-b]pyrimidine-4-one(6a)and 1-aryl-1, 2, 3-triazo-lo[4, 5-e] azacyclooctane[1, 2-b] pyrimidine-4-one (7a), were prepared by treating l-aryl-4-ethyloxycarbonyl-5-amino-1, 2, 3-triazoles 1 with formamide, chlorosulphonyl isocyanate, lactin respectively. The structures of all compounds were confirmed by elemental analysis, IR, 1H NMRand MS. Their antibacterial activities against B. Subtilis, E. coli, E. aerogenes; S. aureus were observed.

Key words: Condensed heterocyclic compound, 1-Aryl-1,2,3-triazolo[4,5-e] pyrimidineone, 1-Aryl-1,3-triazolo[4,5-e]piperidine[1,2-b] pyrimidine-4-one, 1,3-Triazolo[4,5-e]azacyclooctane[1,2-b]pyrimidine-4-one, Biological activity

TrendMD: