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

摘要

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 synthe-sized by the reaction of 1 wtih substituted amines ( 2 a ~2 i ) .The structures were characterized by 1 H NMR, 13 C 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-me-thoxyphenyl)-3-[3-(trifluoromethyl)phenyl]urea(3c) exhibited best biological activities with auxin activity of 29.8%at dosage of 10 mg· L -1, better thanβ-indoleacetic acid(29.3%).%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％）。