吡唑酰胺基脲类化合物的合成及除草活性

Synthesis and herbicidal activity of some new pyrazolyl amido urea derivatives

摘要: 根据活性结构拼接原理,以1-甲基-3-乙基-5-吡唑甲酰肼为起始原料,设计合成了19个新吡唑酰胺基脲类衍生物,其结构均经过核磁共振氢谱、红外光谱、质谱和元素分析确证。生物活性测试结果表明:大部分化合物对双子叶杂草苘麻Abutilon theophrasti、反枝苋Amaranthus retroflexus以及凹头苋A.ascedense显示出较好的除草活性及选择性,如在2 250 g/hm2的剂量下,3i在苗后和苗前处理时,对苘麻和反枝苋的抑制率都达到了100%。复筛的结果表明,在375 g/hm2下,3i对双子叶杂草表现出中等除草活性。

Abstract: A new series of amido ureas were synthesized from the 3-ethyl-1-methyl-5-hydrazinocarbonylpyrazole and substituted phenyl isocyanate.Their structures were confirmed by 1H NMR,FTIR,MS and elemental analysis.The herbicidal activity of these compounds was evaluated.The results showed that most of them exhibited higher herbicidal activity against dicotyledonous weeds than that of monocotyledonous weeds.For example,compound 3i had 100% inhibitory effect against Abutilon theophrasti and Amaranthus retroflexus at 2 250 g/ha in post-emergence and pre-emergence condition.Compound 3i had also moderate inhibitory effect against dicotyledonous weeds at the dose of 375 g/ha.