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为了研究邻甲酰胺基苯甲酰胺类化合物的杀虫活性,总结该类化合物的构效关系、合成高活性化合物,以2-氨基-3-羟基丙酸与取代2-硝基苯甲酸为原料,经过酯化反应、缩合反应、硝基还原反应、三光气缩合反应等一系列步骤,合成了29个2-(取代苯基)噁唑基的邻甲酰胺基苯甲酰胺类目标化合物,产率在30%~50%之间.根据离体杀东方粘虫活性测定实验结果可知,该类化合物对东方粘虫表现出一定的杀虫活性,其中目标化合物2-(2-溴苯基)-N-(4-氯-2-甲基氨基甲酰基-6-甲基苯基)噁唑-4-甲酰胺(11p)活性最高.通过对目标化合物的结构与杀虫活性的分析,总结出该类化合物的构效关系,筛选出了较高活性的目标化合物.
In order to study the insecticidal activity of o-formamidobenzamides, the structure-activity relationship of these compounds was summarized and the highly active compounds were synthesized. Using 2-amino-3-hydroxypropionic acid and substituted 2-nitrobenzoic acid as raw materials , A series of 29 2- (substituted phenyl) oxazolyl o-formamidobenzamides were synthesized through a series of steps such as esterification, condensation, nitro reduction and triphosgene condensation. The rate was between 30% and 50% .According to the results of the in vitro test of activity against Mythimna separata, it was found that the compounds exhibited some insecticidal activity against Mythimna separata and the target compound 2- (2-bromophenyl) (4-chloro-2-methylcarbamoyl-6-methylphenyl) oxazole-4-carboxamide (11p) was the most active.According to the analysis of the structure and insecticidal activity of the target compounds, The structure-activity relationship of these compounds was screened out and the higher activity of the target compounds was screened out.