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有机化学
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有机化学 ›› 2005, Vol. 25 ›› Issue (11): 1498-1502. 上一篇    

研究简报

5,7-二甲基-1,2,4-三唑并[1,5-a]嘧啶-2-甲酰腙类化合物的合成与生物活性

龙德清*,1，汪焱钢2，李德江1，王锋尖1   

  1. (1郧阳师范高等专科学校化学系 丹江口 442700)
    (2华中师范大学化学学院 武汉 430079)
  • 收稿日期:2005-08-17 修回日期:2005-09-14 发布日期:2005-10-30
  • 通讯作者: 龙德清

Synthesis and Biological Activity of 2-Benzylidenehydrazinocar-bonyl-5,7-dimethyl-1,2,4-triazolo[1,5-a]pyrimidine

LONG De-Qing*,1,WANG Yan-Gang2,LI De-Jiang1,WANG Feng-Jian1   

  1. (1 Department of Chemistry, Yunyang Teachers College, Danjiangkou 442700)
    (2 College of Chemistry, Central China Normal University, Wuhan 430079)
  • Received:2005-08-17 Revised:2005-09-14 Published:2005-10-30
  • Contact: LONG De-Qing

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以5-氨基-1H-1,2,4-三唑-3-羧酸为起始原料, 设计合成了13个新型的5,7-二甲基-1,2,4-三唑并[1,5-a]嘧啶-2-甲酰腙类化合物, 通过1H NMR, MS和元素分析对所合成的化合物进行了结构表征. 初步的生物活性测试结果表明, 所合成的化合物均表现出不同程度的除草及杀菌活性, 其中化合物4b, 4h和5m的活性较好, 在50 mg/L浓度下对水稻纹枯病菌的抑制率达90 %以上.

关键词: 1,2,4-三唑并[1,5-a]嘧啶, 甲酰腙, 合成, 生物活性

Thirteen novel 2-benzylidenehydrazinocarbonyl-5,7-dimethyl-1,2,4-triazolo[5,1-a]pyrimidine derivatives were designed and synthesized by using 5-amino-1,2,4-triazole-3-carboxylic acid as a starting material. All compounds synthesized were confirmed by 1H NMR, MS spectra and elemental analyses. Preliminary bioassay indicates that some compounds display herbicidal activity and excellent fungicidal activity to some extent, among them the compounds 5b, 5h and 5m exhibited higher than 90% inhibition effect against Rhizoctonia solani in dosage of 50 mg/L.

Key words: carbonylhydrazone, synthesis, biological activity, 1,2,4-triazolo[1,5]-a]pyrimidine