为了研究丙硫菌唑高生物活性的1，2，4-三氮唑衍生物，以丙硫菌唑关键中间体1-氯-1-氯乙酰基环丙烷为原料，经过2步亲核取代、还原和亲电加成反应设计合成了1，2，4-三氮唑衍生物，并确定了其最佳反应条件。在最佳反应条件下制得目标产物1-（1-氯-环丙基）-3-（2-氟-苯基）-2-（5-硫代-2，5-二氢-[1，2，4]三唑）-1-丙醇，产物的总收率（以1-氯-1-氯乙酰基环丙烷计）为23.4%。

In order to study a 1,2,4-triazole derivative with high biological activity that is similar with prothioconazole,1-chloro-1-chloroacetyl cyclopropane,a key intermediate for rothioconazole,is used as raw material to synthesis 1,2,4-triazole derivative through a four-step reaction including two-step nucleophilic substitution,reduction and electrophilic addition.The optimal reaction conditions are determined.Under the optimal reaction conditions,1-(1-chlorine-cyclopropyl)-3-(2-fluoro-phenyl)-2-(5-thio-2,5-dihydro-[1,2,4-trichlorobenzene] triazole)-1-propanol is synthesized.The overall yield counting on 1-chloro-1-chloroacetyl cyclopropane is 23.4%.

单俊(1991-),男,硕士研究生,研究方向为精细有机合成,1520523411@qq.com。