以2-N,N-二乙胺基-4-氯-硝基RM(1)为起始原料,通过取代、催化还原和酰化等反应,设计合成了13个结构中含有氧醚和烷胺侧链的多取代嘧啶-氨基酰胺及芳基(硫)脲衍生物(4),通过1H NMR,MS和元素分析确证了化合物的结构.生物活性测试结果表明,所有化合物均显示出良好的抗烟草花叶病毒活性,其中化合物41的活性高于相同浓度下阳性对照药剂病毒唑.%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 , which makes it more reachable to design and synthesis 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 with high yields using 2-./V,7V-diethyl-amino-4-chloro-5-nitropyrimidine(l) as starting material via substitution, reduction and acylation procedures in turn. The bioassay results indicate that nearly all the target compounds process good anti-TMV activity, but no herbicidal or fungicidal activities. Among them, compound 41 exhibits the highest inhibition value, which is higher than that of the positive control virazole ( ribavirin) at the same concentration.
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