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化学学报
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化学学报 ›› 2004, Vol. 62 ›› Issue (2): 204-207. 上一篇    下一篇

研究论文

相转移催化合成吡啶三唑并噻二唑及舒张血管活性研究

胡国强1, 张忠泉1, 许启泰1, 黄文龙2, 汪海3   

  1. 1. 河南大学药学院, 开封, 475001;
    2. 中国药科大学新药中心, 南京, 210009;
    3. 军事医学科学院毒物研究所, 北京, 100850
  • 投稿日期:2003-01-27 修回日期:2003-09-23 发布日期:2014-01-26
  • 通讯作者: 胡国强,许启泰,E-mail:hgqxy@sina.com.cn E-mail:hgqxy@sina.com.cn
  • 基金资助:
    国家重点基础研究发展项目(No.G1998051112)和河南大学科学研究基金(No.XK02043)资助项目.

Phase Transfer Catalyzed Synthesis and Bioactivity of s-Triazolo[3,4-b]thiadiazoles

HU Guo-Qiang1, ZHANG Zhong-Quan1, XU Qi-Tai1, HUANG Wen-Long2, WANG Hai3   

  1. 1. Medical College of Henan University, Kaifeng 475001;
    2. Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009;
    3. Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing 100850
  • Received:2003-01-27 Revised:2003-09-23 Published:2014-01-26

PDF

278

被引次数

122

3-(3-吡啶基)-4-氨基-5-巯基-1,2,4-均三唑(1)与羧酸在相转移催化剂四丁基碘化铵和三氯氧磷催化作用下,高收率制得3-(3-吡啶基)-6-取代-s-1,2,4-三唑并[3,4-b]噻二唑(2a～2s).体外舒血管活性试验表明,大部分化合物具有较好的舒张生理活性.

关键词: 相转移催化, 吡啶均三唑并噻二唑, 合成, 生物活性

A series of 3-(3-pyridyl)-6-substituted-s-1,2,4-triazolo[3,4-b]thiadiazoles was synthesized in good yields via condensation of 3-(3-pyridyl)-4-amino-5-thio-1,2,4-thiazoles with carboxylic acids in the presence of POCl3 and phase transfer catalyst tetrabutylammonium iodide (TBAI). The structures of the target compounds were confirmed by IR, 1H NMR, MS and elemental analyses, and the in vitro activity was also evaluated.

Key words: phase transfer catalysis, pyridyl triazolothiadiazole, synthesis, bioactivity