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林产化学与工业

林产化学与工业 ›› 2011, Vol. 31 ›› Issue (1): 1-8.

• 研究报告 •    下一篇

5-去氢枞基-1,3,4-噻二唑衍生物的合成和除草活性

段文贵1, 李行任1, 马献力1,2, 莫启进1, 许雪棠1, 岑波1   

  1. 1. 广西大学化学化工学院, 广西 南宁530004;2. 广西大学化学化工学院, 广西 南宁530004
  • 收稿日期:2010-07-29 修回日期:1900-01-01 出版日期:2011-02-28 发布日期:2011-02-28

Synthesis and Herbicidal Activity of 5-Dehydroabietyl- 1,3,4-thiadiazole Derivatives

DUAN Wen-gui1, DUAN Wen-gui1, LI Xing-ren1,2, MA Xian-li1, MO Qi-jin1, XU Xue-tang1   

  1. 1. College of Chemistry and Chemical Engineering, Guangxi University, Nanning 530004, China;2. College of Pharmacy, Guilin Medical University, Guilin 541004, China
  • Received:2010-07-29 Revised:1900-01-01 Online:2011-02-28 Published:2011-02-28

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摘要： 为了寻找具有更高生物活性的新颖化合物,设计并合成了具有1,3,4-噻二唑骨架的系列新型去氢枞酸衍生物。在磷酸催化下, 通过中间体1-去氢枞酰基-4-取代基氨基硫脲4(a～h)的关环反应, 合成得到8个目标产物5-去氢枞基-2-取代氨基-1,3,4-噻二唑5(a～h),并采用IR、UV、EI-MS、1HNMR、13CNMR 和元素分析等方法对其进行了分析和表征。初步生物活性测试结果表明:所有这些目标化合物均对油菜(Brassica campestris)表现出良好的抑制作用,对稗草(Echinochloa crusgalli(L.))有一定的抑制活性。

关键词: 去氢枞酸, 4-噻二唑, 合成, 除草活性

Abstract: In order to search for novel compounds with higher biological activity, a series of new dehydro-abietic acid derivatives bearing 1,3,4-thiadiazole moieties were designed and synthesized. Eight title compounds of 5-dehydroabietyl-2-substituted amino-1,3,4-thiadiazoles 5(a-h) were synthesized by the cyclization of 1-dehydroabietacyl-4-substituted thiosemicarbazides 4(a-h) under the catalysis of phosphoric acid. All the title compounds were analyzed and characterized by means of IR, UV, EI-MS,1HNMR,13CNMR, and elemental analysis. The preliminary bioassay showed that all these title compounds exhibited excellent growth inhibition against rape(Brassica campestris) and a certain inhibition against barnyard grass Echinochloa crusgalli(L.).

Key words: dehydroabietic acid, 4-thiadiazole, synthesis, herbicidal activity

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