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新型1-取代-3-(4-甲氧基苯基)脲衍生物的合成及其生物活性

Synthesis and Biological Activities of 1-Substituted-3-( 4-methoxyphenyl) urea Derivatives

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【作者】 严晓阳; 赵胜贤; 孔黎春; 郑绍成;

【Author】 YAN Xiao-yang;ZHAO Sheng-xian;KONG Li-chun;ZHENG Shao-cheng;Xingzhi College,Zhejiang Normal University;Zhejiang Apeloa Tospo Pharmaceutical Co.,Ltd.;College of Chemistry and Life Science,Zhejiang Normal University;

【机构】 浙江师范大学行知学院; 浙江普洛得得邦制药有限公司; 浙江师范大学化学与生命科学学院;

【摘要】 以对甲氧基苯胺和固体三光气为起始原料,制得4-甲氧基苯异氰酸酯(1);1与取代胺(2a~2i)反应合成了9个新型的1-取代-3-(4-甲氧基苯基)脲衍生物(3a~3i),其结构经1H NMR,13C NMR和HR-MS表征。用黄瓜子叶扩张法和小麦芽鞘法研究了3a~3i的生物活性。结果表明:1-(4-甲氧基苯基)-3-[3-(三氟甲基)苯基]脲(3c)的生长素活性最好。在用药浓度为10 mg·L-1时,3c的生长素活性为29.8%,优于β-吲哚乙酸(29.3%)。

【Abstract】 1-Isocyanato-4-methoxybenzene( 1) was prepared by the reaction of methoxyaniline with triphosgene. Nine novel 1-substituted-3-( 4-methoxy-phenyl) urea derivatives( 3a 3i) were synthesized by the reaction of 1 wtih substituted amines( 2a 2i). The structures were characterized by 1 H NMR,13C NMR and HR-MS. The biological activities of 3a 3i were investigated by cucumber cotyledon expansion method and wheat sprout and sheath method. The results showed that 1-( 4-methoxyphenyl)-3-[3-( trifluoromethyl) phenyl]urea( 3c) exhibited best biological activities with auxin activity of 29. 8% at dosage of 10 mg·L-1,better than β-indoleacetic acid( 29. 3%).

  • 【文献出处】 合成化学 ,Chinese Journal of Synthetic Chemistry , 编辑部邮箱 ,2016年08期
  • 【分类号】O621.3
  • 【被引频次】1
  • 【下载频次】95
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