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N-(4,6-二甲氧基嘧啶-2-基)-N'-磷酰基脲类衍生物的合成及生物活性
引用本文:赵国锋,杨华铮,王玲秀. N-(4,6-二甲氧基嘧啶-2-基)-N'-磷酰基脲类衍生物的合成及生物活性[J]. 高等学校化学学报, 1998, 19(4): 555-559
作者姓名:赵国锋  杨华铮  王玲秀
作者单位:南开大学元素有机化学研究所, 元素有机化学国家重点实验室, 天津, 300071
摘    要:利用二氯代磷酰基异氰酸酯与4,6-二甲氧基-2-氨基嘧啶的加成反应合成了中间体N-(4,6-二甲氧基嘧啶-2-基)-N'-二氯代磷酰基脲(Ⅰ).Ⅰ与2倍的醇或胺反应得到对称双取代磷酰基脲类化合物Ⅱa_Ⅱi;Ⅰ与1倍的胺反应得到氯代磷酰基脲类化合物Ⅲa_Ⅲe,再与1倍的醇反应则得到不对称双取代磷酰基脲类化合物Ⅳa_Ⅳg.生物活性测定结果表明,化合物Ⅱ、Ⅲ和Ⅳ均显示一定除草活性.

关 键 词:磷酰基脲  加成反应  合成  生物活性  
收稿时间:1997-01-20
修稿时间:1997-01-20

The Synthesis and Biological Activity of N-(4,6-Dimethoxy-2-pyrimidinyl)-N'-phosphoryl Urea Derivatives
ZHAO Guo-Feng,YANG Hua-Zheng,WANG Ling-Xiu. The Synthesis and Biological Activity of N-(4,6-Dimethoxy-2-pyrimidinyl)-N'-phosphoryl Urea Derivatives[J]. Chemical Research In Chinese Universities, 1998, 19(4): 555-559
Authors:ZHAO Guo-Feng  YANG Hua-Zheng  WANG Ling-Xiu
Affiliation:Institute of Elemento Organic Chemistry, National Key Laboratory of Elemento Organic Chemistry, Nankai University, Tianjin, 300071
Abstract:In this paper N-(4,6-dimethoxY-2-pyrimidinyl)-N'-dichloro-phosphoryl urea(Ⅰ) was synthesized by addition reaction of dichloro phosphoryl isocyanate with 4,6-dimethoxY-2-aminopyrimidine. Compound Ⅰ reacted with two equivalents of amines or alcohols to obtain symmetric disubstituted phosphoryl urea derivatives Ⅱa_Ⅱi, and reacted with one equivalent of amines to give monochlorophosphoryl ureas Ⅲa_Ⅲe which reacted with one equivalent of alcohols to obtain asymmetric disubstituted phosphoryl urea derivatives Ⅳa_ Ⅳg. The biological tests indicated that compounds Ⅱ, Ⅲ and Ⅳ showed herbicidal activities.
Keywords:Phosphoryl urea   Addition reaction   Synthesis   Biological activity
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