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

The Synthesis and Biological Activity of N (4,6 Dimethoxy 2 pyrimidinyl) N  phosphoryl Urea Derivatives

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．

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.