高等学校化学学报 ›› 1998, Vol. 19 ›› Issue (4): 555.

• 论文 • 上一篇    下一篇

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

赵国锋, 杨华铮, 王玲秀   

  1. 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
  • 收稿日期:1997-01-20 出版日期:1998-04-24 发布日期:1998-04-24
  • 通讯作者: 杨华铮
  • 作者简介:赵国锋,男,30岁,博士,副研究员.
  • 基金资助:

    国家自然科学基金

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   

  1. Institute of Elemento Organic Chemistry, National Key Laboratory of Elemento Organic Chemistry, Nankai University, Tianjin, 300071
  • Received:1997-01-20 Online:1998-04-24 Published:1998-04-24

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

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.

Key words: Phosphoryl urea, Addition reaction, Synthesis, Biological activity

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