1-[2-(2,4-二氯苯氧)乙酰基]-5-氨基-1H-吡唑衍生物的合成与生物活性

Synthesis and Biological Activity of 1-[2-(2,4-Dichlorophenoxyl)acetyl]- 5-amino-1H-pyrazole Derivatives

为寻求高效低毒的农药 ,设计、合成了一系列新的 1 [2 ( 2 ,4 二氯苯氧 )乙酰基 ] 5 氨基 1H 吡唑衍生物 3a～ 3j和4a～ 4d.元素分析 ,1HNMR ,IR和MS证实了它们的结构 .初步的生物活性测试结果表明 ,在 1 0mg/L浓度下 ,化合物 3a～3j和 4a～4d对油菜的根茎均有很好的抑制作用 ,对油菜的根的抑制率为 90 .0 %～ 98.7% ;于 1 0 0mg/L浓度下 ,对稗草的根抑制率为 84.0 %～1 0 0 % .

In an attempt to discover novel compounds with high activity and low toxicity, a series of new 1-[2-(2,4-dichlorophenoxyl) acetyl]-5-amino-1H-pyrazole derivatives 3a similar to 3j and 4a similar to 4d have been designed and synthesized by the reaction of 2,4-dichlorophenoxylacetyl chloride with 5-amino-1H-pyrazole. The structures of all new compounds were confirmed by elemental analyses, H-1 NMR, IR and MS spectroscopies. The results of preliminary bioassay indicate that compounds 3a similar to 3j and 4a similar to 4d possess high herbicidal activity against the root of rape and barnyard grass.