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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。
According to the principle of active structure splicing, 19 novel pyrazoloylaminoureas derivatives were designed and synthesized with 1-methyl-3-ethyl-5-pyrazole carboxylic acid hydrazide and their structures were all confirmed by NMR Hydrogen, infrared, mass spectrometry and elemental analysis confirmed. The results of bioassay showed that most of the compounds showed good herbicidal activity and selectivity to Abutilon theophrasti, Amaranthus retroflexus and A.ascedense. For example, in the range of 2 250 g / hm2 At the dose of 3i, the inhibitory rate of 3i in both post-emergence and pre-emergence treatments reached 100%. Screening results showed that 3i showed moderate herbicidal activity against dicotyledonous weeds at 375 g / hm2.