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有机化学 ›› 2012, Vol. 32 ›› Issue (08): 1513-1518.DOI: 10.6023/cjoc1201041 上一篇    下一篇

研究简报

α-(1-苯基-3-三氟甲基-5-氯吡唑-4-甲酰氧基)-α-芳甲基膦酸酯的合成、晶体结构与生物活性

梁英a,b, 贺红武b, 何海峰a,b, 杨自文a   

  1. a 湖北省农业科学院 湖北省生物农药工程研究中心 武汉 430064;
    b 华中师范大学化学学院 教育部农药与化学生物学重点实验室 武汉 430079
  • 收稿日期:2012-01-04 修回日期:2012-03-12 发布日期:2012-04-27
  • 通讯作者: 贺红武 E-mail:he1208@mail.ccnu.edu.cn
  • 基金资助:

    国家自然科学基金(Nos. 20772042, 31000867)资助项目.

Synthesis, Crystal Structure and Biological Activity of α-(5-Chloro- 3-trifluoromethyl-1-phenylpyrazol-4-carbonyloxy)-α- arylmethyl Phosphonates

Liang Yinga,b, He Hongwub, He Haifenga,b, Yang Ziwena   

  1. a Hubei Biopesticide Engineering Research Center, Hubei Academy of Agricultural Science, Wuhan 430064;
    b Key Laboratory of Pesticide and Chemical Biology of Ministry of Education, Central China Normal University, Wuhan 430079
  • Received:2012-01-04 Revised:2012-03-12 Published:2012-04-27
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 20772042, 31000867).

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通过1-苯基-3-三氟甲基-5-氯吡唑-4-甲酰氯(4)与α-羟基芳甲基膦酸酯(6)的缩合反应, 合成了14种标题化合物7a～7n. 所有化合物的结构均经1H NMR, IR和元素分析进行了表征, 并且采用X射线单晶衍射分析方法进一步测定了化合物7j的结构. 初步的生物活性测试表明, 部分标题化合物具有一定的杀菌和除草活性.

关键词: 芳甲基膦酸酯, 合成, 晶体结构, 生物活性

Fourteen novel α-(substituted pyrazol-4-carbonyloxy)-α-arylmethyl phosphonates 7a～7n were synthesized from the intermediates 5-chloro-3-trifluoromethyl-1-phenylpyrazol-4-carbonyl chloride (4) and α-hydroxyl-α-arylmethyl phos- phonates (6). All compounds synthesized were identified by 1H NMR, IR spectra and elemental analysis, and the structure of 7j was further determined by X-ray single crystal diffraction method. The preliminary bioassay indicated that some compounds showed moderate fungicidal and herbicidal activities.

Key words: arylmethylphosphonate, synthesis, crystal structure, bioactivity