含氟代吡唑环的双酰肼类化合物的合成及除草活性有机化学.pdfVIP

2011 年第 31 卷 有 机 化 学 Vol. 31, 2011 第 8 期, 1295～1299 Chinese Journal of Organic Chemistry No. 8, 1295～1299 ·研究简报· 含氟代吡唑环的双酰肼类化合物的合成及除草活性 * 张向阳 李永曙 翁建全 谭成侠 (浙江工业大学化学工程与材料学院 杭州 310014) 摘要 根据活性亚结构拼接原理, 将含氟吡唑环引入到双酰肼结构中, 设计并合成了 19 个未见文献报道的含氟吡唑双 酰肼类衍生物, 其结构均经过 1H NMR, FTIR, MS 和元素分析确证, 同时对所有化合物进行了除草活性的测试. 生物活 性测试结果表明, 大部分化合物对双子叶杂草苘麻、反枝苋以及凹头苋显示出较好的除草活性及选择性. 关键词 含氟吡唑; 双酰肼; 合成; 除草活性 Synthesis and Herbicidal Activity of Some New Diacylhydrazine Derivatives Fluoride-Containing Pyrazolyl Moiety Zhang, Xiangyang Li, Yongshu Weng, Jianquan Tan, Chengxia* (College of Chemical Engineering and Materials Science, Zhejiang University of Technology, Hangzhou 310014) Abstract In search of novel bioactive compounds, compounds 3a～3s were designed and synthesized by introducing the fluoropyrazolyl pharmacophore into the diacylhydrazine scaffold. Their structures were con- 1 firmed by H NMR, FTIR, MS techniques and elemental analysis. The herbicidal activities of these com- pounds were evaluated. The bioassay results showed that most of them exhibited higher herbicidal activities against dicotyledonous weeds (Abutilon theophrasti , Amaranthus ascedense and Amaranthus retroflexus) than monocotyledonous weeds. Keywords fluoride pyrazole; diacylhydrazine; synthesis; herbicidal activity 双酰肼类化合物由于其低毒、高敏感性和独特的作 中, 设计并合成了一系列含氟吡唑双酰肼类化合物, 其 用模式已经发展成为一类昆虫生长调节剂[1,2], 如抑食 结构均经过 1H NMR, FTIR, MS 和元素