Chem. J. Chinese Universities ›› 2011, Vol. 32 ›› Issue (7): 1545.

• Preface • Previous Articles     Next Articles

Synthesis and Anti-TMV Activity of Novel Poly-substituted Pyrimidine-5-amino Amide and Aryl(Thio)urea Derivatives

XU Wei-Pan1, ZHANG Da-Qiang1, LI Ru-Xing2, YANG Xin-Ling1, WANG Dao-Quan1, YUAN De-Kai1*, FAN Zhi-Jin3   

  1. 1. Science College, China Agricultural University, Beijing 100191, China;
    2. Beijing Double-crane Pharmaceutical Co., Ltd., Beijing 100102, China;
    3. State Key Laboratry of Elemento-Organic Chemistry, Institute of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, China
  • Received:2010-08-17 Revised:2011-01-06 Online:2011-07-10 Published:2011-06-02
  • Contact: YUAN De-Kai E-mail:yuandekai@yahoo.com.cn
  • Supported by:

    国家自然科学基金(批准号: 20672138, 20902107)、 科技部“十一五”科技支撑计划项目(批准号:  2006BAE01A01-1104)和中央高校基本科研业务费专项资金项目(批准号: 2011JS033)资助.

Abstract: Pyrimidine plays important roles in pesticide innovation research and pyrimidine sub-structure can be easily found in fungicides, herbicides and insecticides or miticides, etc. As this ring can be easily modified, that makes it more reachable to design and synthesis of novel bio-active heterocycle compounds from some pyrimidine structures. Based on our previous studies on pyrimidine and purine, three series of novel poly-substituted pyrimindine 5-amino derivatives (4) were designed and obtained in high yields by using 2-N,N-diethylamino-4-chloro-5-nitropyrimidine (1) as starting material via substitution, reduction and acylation procedures in turn. The priliminary bioassay results indicate that nearly all the target compounds processing good anti-TMV activity, but no herbicidal or fungicidal activities. Among them, compound 4l exhibits the highest inhibition value, which is higher than that of the positive control virazole (ribavirin) at the same concentration.

Key words: 2-N,N-Diethylamino-4-chloro-5-nitropyrimidine, Synthesis, Pyrimidine-5-amino derivatives, Anti-TMV activity

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