N-甲基邻苯酰胺基苯甲酰胺衍生物的合成

Synthesis of N-substituted Anthranilic Diamides Derivatives

为了获得结构简单、合成步骤少、收率高的邻苯酰胺类杀虫剂,首先以2-氨基苯甲酸甲酯与硫酸二甲酯为起始原料进行N-甲基化反应,再与不同酰氯进行酰胺化反应,然后在碱性条件下水解得到2-芳酰胺基苯甲酸.将2-芳酰胺基苯甲酸与不同的芳胺反应得到5个邻苯酰胺基苯甲酰胺衍生物.所有化合物经核磁共振氢谱以及质谱表征,波谱数据与衍生物吻合.结果表明,这种合成邻苯酰胺基苯甲酰胺衍生物的方法是可行的,为杀虫剂的进一步筛选研究奠定了基础.

To obtain the amide pesticide with simple structures, less synthesis steps and high yield, we synthesized the 2-aromatic amide benzoic acid by N-methylation, amidation and ester hydrolysis method using methyl anthranilate and dimethylsulfate as raw materials. Then, the five N-substituted anthranilic diamides derivatives were prepared by the reaction of 2-aromatic amide benzoic acid with different aromatic amines. And their structures were confirmed by proton nuclear magnetic resonance spectroscopy and mass spectrometry. The results show that this synthesis method is feasible, which lays a foundation for further screening of insecticides.