论文部分内容阅读
[方法]为寻找高活性的杀螨剂,以乙螨唑为先导化合物,以2,6-二氟苯甲酸为起始原料,经过碘代、酰氯化、氨解得到3-碘-2,6-二氟苯甲酰胺(4),中间体4经过缩合反应、傅克烷基化、关环反应,最后与有机硼酸发生Suzuki偶联反应合成了系列乙螨唑衍生物,其结构经元素分析及核磁共振氢谱分析确证。[结果]生物活性测试结果表明绝大多数新化合物对朱砂叶螨螨卵表现出了较高的生物活性。[结论]通过构效关系分析得知:苯硼酸以及3位吡啶硼酸所合成的衍生物普遍表现出较高的生物活性。
[Method] In order to find highly active acaricides, etidronate was used as the lead compound and 2,6-difluorobenzoic acid as the starting material. After iodination, acid chlorination and aminolysis, 3-iodo- A series of Ertesol derivatives were synthesized by Suzuki coupling reaction with organic boronic acid through condensation reaction, Friedel-Crafts alkylation and ring-closure reaction. The structures of the compounds were characterized by elemental analysis and Nuclear magnetic resonance 1H NMR analysis confirmed. [Result] The results of biological activity tests showed that most of the new compounds showed high biological activity on the eggs of Tetranychus cinnabarinus. [Conclusion] The structure-activity relationship analysis showed that the derivatives synthesized by benzene boronic acid and 3-position pyridine boronic acid generally showed higher biological activity.