嘧啶酮类衍生物的合成及杀虫活性

为了创制高效广谱的绿色杀虫剂,以(E)-4,5-二氢-6-甲基-4-(3-吡啶亚甲基氨基)-1,2,4-三嗪-3(2H)-酮(吡蚜酮)为先导,用带有不同电荷密度的五元、六元取代苯环或杂环取代其结构中的吡啶环部分,合成了10个全新的嘧啶酮类衍生物,特别对其中所包含的三嗪环和二氢喹唑啉酮合成部分进行了重点研究。所有目标化合物的结构均经过核磁共振氢谱、高分辨质谱及红外光谱的确认。初步杀虫活性测试结果表明,目标化合物对蚜虫Aphis craccivora未表现出明显的杀虫活性,初步暗示了先导化合物吡蚜酮结构中所含的吡啶环部分可能对其杀虫活性起了重要作用。

Synthesis and insecticidal activity of pyrimidone derivatives

In order to find high activity and broad-spectrum insecticide,ten novel pyrimidone derivatives were designed via the replacement of pyridine ring of pymetrozine with the different charge density five-or six-membered rings.A facile and efficient synthetic method for the preparation of pyrimidone derivatives was described,in which the triazone ring and dihydroquinazolin-2( 1H)-one was conveniently constructed.The structures of all the newly synthesized compounds were characterized by HRMS,1H NMR and IR spectroscopy.The insecticidal activity tests showed that these compounds didn’t exhibit significant insecticidal activity against Aphid scraccivora,which implied that the pyridine ring moiety of pyrimidone is essential for its insecticidal activity.