2-(4-氯苯基)-1-(1H-1,2,4-三唑-1-基)-2-丁醇的合成研究

Synthesis of 2-(4-chloro benzyl)-1-(1H-1,2,4-triazole-1-)-2-butanol

唑醇类杀菌剂对植物的常见致病菌如鞭毛菌、担子菌、半知菌等均有很好的预防和治疗作用,在农药领域应用十分广泛。以对氯苯丙酮为原料,经Corey-Chaykovsky环氧化,再与1H-1,2,4-三氮唑缩合,合成了唑醇化合物2-(4-氯苯基)-1-(1H-1,2,4-三唑-1-基)-2-丁醇。探讨了环氧化反应的关键因素,收率可达97.9%。对缩合反应条件进行了正交优化:以碳酸氢钠为碱催化剂,环氧化物、1H-1,2,4-三氮唑、碳酸氢钠的摩尔比为1.0∶1.5∶2.1,反应温度130℃,反应5 h,缩合收率可稳定在82.0%以上。

Triazole alcohols are used widely as disinfectants to prevent and treat the common pathogenic bacteria in plants,such as whip trichobacteria,basidiomycetes,imperfect fungi and so on.2-（4-chlorine benzyl）-1-（1H-1,2,4-triazole-1-）-2-butylacohol was synthesized by Corey epoxidation from p-chloro benzene acetone,and by condensation with the 1H-1,2,4-triazole.The factors influencing the Corey-Chaykovsky epoxidation were studied and the yield was 97.9%.The optimum technological conditions of condensation were determined through orthogonal experiments.The optimum reaction conditions required that the molar ratio of the epoxide,1H-1,2,4-triazole,and sodium bicarbonate was 1.0∶1.5∶2.1,the reaction temperature was 130℃,and the reaction time was 5 h.The condensation yield was above 82.0%.