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以丁酮、草酸二乙酯为原料,经Claisen缩合、Knorr环合和甲基化等多步反应合成了8个结构新颖的1-甲基-1H-吡唑-5-甲酰胺类化合物,其结构经Mass和1H NMR等确证。生测结果表明:化合物7a和7g在200 mg/L浓度下,对蚜虫表现出95%以上的活性;而化合物7h在100 mg/L浓度下,对小麦白粉病菌具有73.8%的防治效果。
Eight novel 1-methyl-1H-pyrazole-5-carboxamides were synthesized from methyl ethyl ketone and diethyl oxalate by Claisen condensation, Knorr cyclization and methylation. Its structure confirmed by Mass and 1H NMR. The results of bioassay showed that compounds 7a and 7g showed more than 95% activity against aphids at the concentration of 200 mg / L, while compound 7h had 73.8% control effect on powdery mildew at 100 mg / L.