杀菌剂苯醚甲环唑的制备

Preparation of Fungicide Difenoconazole

  • 摘要: 研究杀菌剂苯醚甲环唑的制备.以2,4-二氯苯乙酮为起始原料,经醚化、溴化、缩酮化、亲核取代4步反应制得苯醚甲环唑.醚化反应采用一步法,酚的成盐与醚化反应同时进行,收率可达93.6%.在醚化产物(Ⅲ)的甲基上进行溴化反应得到溴化产物(Ⅳ),产率89.1%.化合物(Ⅳ)与1,2-丙二醇反应得到缩酮产物(Ⅴ),产率89.6%.化合物(Ⅴ)与1H-1,2,4-三氮唑进行亲核取代反应得到目标产物(Ⅵ),产率69.0%.对各步反应的工艺进行了改进,总收率高达51.6%.

     

    Abstract: The preparation of fungicide difenoconazole is studied.Difenoconazole was prepared from(2,4-dichloroacetophenone) followed by etherification,bromination,ketal reaction and nucleophilic substitution.Phenol salt formation and etherification were finished in one step pathway to give(Ⅲ) in 93.6% yield.Bromination of(Ⅲ) with bromine gave(Ⅳ) in 89.1% yield.The compound(Ⅴ) was obtained by ketal reaction of(Ⅳ) with 1,2-propylene glycol in 89.6% yield.The title compound(Ⅵ) was then prepared by nucleophilic substitution of(Ⅴ) with 1H-1,2,4-triazole in 69.0% yield.The procedure was eventually improved and the total yield reached 51.6%.

     

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