关键词: 2-N,N-二乙胺基-4-氯-5-硝基嘧啶, 合成, 嘧啶-5-氨基衍生物, 抗烟草花叶病毒活性

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