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O-烷基硫代磷酰二氯与相应的取代酚在氢氧化钠及少量三乙胺存在下,进行反应.生成O-烷基O-芳基硫代磷酰氯.后者再与胺作用,即得高收率的O-烷基O-芳基硫代磷酰胺.通过所制备化合物苯环上取代基的亲脂性,电性及空间效应参数,研究了该类化合物对于抑制稗草生长的化学结构与活性关系.经回归分析,所得该类化合物的结构与活性的初步关系式如下: pI_(50)=-1.2223π~2+1.2847π-1.0214σ-0.3698E_s+2.4022F+4.0780n=17 Υ=0.9075 s=0.6134同时采用逆相薄层层析法所求得的R_m值,亦可用于反映该类化合物取代基亲脂性的变化.
O-alkylthiophosphoryl dichloride is reacted with the corresponding substituted phenol in the presence of sodium hydroxide and a small amount of triethylamine to form O-alkyl O-arylthiophosphoryl chloride which, in turn, reacts with the amine , To obtain a high yield of O-alkyl O-arylthiophosphoramidites.According to the lipophilicity, electrical and space effect parameters of substituents on the benzene ring of the prepared compounds, the compounds were studied for inhibiting the growth of barnyardgrass Of the chemical structure and activity of the relationship between the structure of the compounds obtained by the regression analysis and activity of the initial relationship is as follows: pI_ (50) = - 1.2223π ~ 2 + 1.2847π-1.0214σ-0.3698E_s + 2.4022F + 4.0780n = 17 Υ = 0.9075 s = 0.6134 The value of Rm obtained by reverse phase thin-layer chromatography can also be used to reflect the change of the lipophilicity of the substituents of these compounds.