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有机化学
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有机化学 ›› 2009, Vol. 29 ›› Issue (06): 924-928. 上一篇    下一篇

研究论文

6-烷基-7-亚胺基-2-硫代-2,3,6,7-四氢噻唑并[4,5-d]嘧啶的合成、晶体结构与生物活性

梁 英a,b ; 贺红武*,a   

  1. (a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)
    (b湖北省农业科学院 湖北省生物农药工程研究中心 武汉 430064)
  • 收稿日期:2008-09-18 修回日期:2008-12-12 发布日期:2009-06-20
  • 通讯作者: 贺红武

Synthesis, Crystal Structure and Biological Activity of 6-Alkyl-7-imino-3- phenyl-2-thioxo-2,3,6,7-tetrahydrothiazolo[4,5-d]pyrimidines

Liang, Ying a,b ; He, Hongwu*,a   

  1. (a Key Laboratory of Pesticide and Chemical Biology, Ministry of Education, Central China Normal University,
    Wuhan 430079)
    (b Hubei Biopesticide Engineering Research Center, Hubei Academy of Agricultural Science, Wuhan 430064)
  • Received:2008-09-18 Revised:2008-12-12 Published:2009-06-20
  • Contact: He, Hongwu

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被引次数

5

通过3-苯基-5-氰基-2-硫代-2,3-二氢-4-乙氧亚甲胺基噻唑(5)与伯胺反应, 经中间体甲脒关环, 合成了10种新的噻唑并[4,5-d]嘧啶类化合物6a～6j. 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6i的结构. 初步的生物活性试验表明, 部分标题化合物具有一定的杀菌或除草活性.

关键词: 合成, 晶体结构, 生物活性, 噻唑并[4,5-d]嘧啶

Ten novel thiazolo[4,5-d]pyrimidines 6a～6j have been synthesized by the reaction of 5-cyano-3-phenyl-2-thioxo-2,3-dihydro-4-ethoxymethylideneaminothiazole (5) with amines via intramolecular cyclization of formamidines. Their structures were characterized by 1H NMR, IR spectra and elemental analysis, and the structure of 6i was further determined by an X-ray single crystal diffraction method. The preliminary bioassay indicated that some compounds showed moderate fungicidal or herbicidal activities.

Key words: synthesis, crystal structure, biological activity, thiazolo[4,5-d]pyrimidine