手性烯唑醇为活性组分的杀菌聚合物的合成

以杀菌剂烯唑醇（Ⅰ）为底物，（-）-孟氧基乙酸为拆分试剂进行手性拆分，得到具有高杀菌活性的（R）-（E）-1-（2，4-二氯苯基）-2-（1，2，4-三唑-1-基）-4，4-二甲基-1-戊烯-3-醇（Ⅱ）。Ⅱ与丙烯酰氯反应生成了具有生物活性的可聚合单体（R）-（E）-1-（2，4-二氯苯基）-2-（1，2，4-三唑-1-基）-4，4-二甲基-1-戊烯-3-醇丙烯酸酯（Ⅲ），Ⅲ经自聚或与丙烯酸或甲基丙烯酸甲酯共聚制得了杀菌聚合物（Ⅳ，Ⅴ，Ⅵ），并进行聚合物活性组分的水解释放实验。总体上，在碱性介质中聚合物的活性组分水解释放速率大于在中性或弱酸性介质中的。Ⅳ和Ⅵ活性组分水解释放速率很低，而聚合物Ⅴ，随时间的延长，有大量的活性组分释出，初始释出质量浓度也较高，符合农用杀菌剂的速效性和持效性的要求，有实用意义。

Syntheses of Fungicide-polymers Containing Chiral Diniconazole

(R)-(E)-1-(2,4-Dichlorophenyl)-2-(1,2,4-triazol-1-yl)-4,4-dimethyl-1-penten-3-ol (II) was synthesizedby resolution of the diastereomer esters obtained from diniconazole (I) and (-)-menthoxyacetyl acid, then the bioactivemonomer, (R)-(E)-1-(2,4-dichlorophenyl)-2-(1,2,4-triazol-1-yl)-4,4-dimethyl-1-penten-3-ol-acrylate (III), was syn-thesized by reacting II with acryloyl chloride, and the fungicide-polymers (IV, V, VI) containing II were obtained bythe radical polymerization of III and copolymerization of III with acrylic acid or methyl methacrylate. The hydrolysisresults of the fungicide-polymers showed that the release rate of active ingredients in a basic medium is higher than ina neutral or acidic medium. It was also indicated that V was characterized by a rapid initial release in the first few daysfollowed by a more gradual rate lasting several weeks and was potentially useful for the development of the commercialCRFs of pesticides, while IV and VI had much lower release rates with little initial release.