布帕伐醌的改进合成方法  

An Improved Synthetic Method of Buparavone

作　　者：袁昊林 赵彦梁 范东升 杨阳 贺万丽 赵佩佩[4] 蔡岩[3,4] Yuan Haolin;Zhao Yanliang;Fan Dongsheng;Yang Yang;He Wanli;Zhao Peipei;Cai Yan(Tianjin International Joint Academy of Biomedicine,Tianjin,300457;College of Pharmacy,Nankai University,Tianjin,300071;College of Chemistry and Environmental Sciences,Kashgar University,Kashgar,844006;Institute of Cangzhou Bohai New Area Green Chemical Engineering,Nankai University,Cangzhou,061100)

机构地区：[1]南开大学药学院,天津300071 [2]喀什大学化学与环境科学学院,喀什844006 [3]南开大学沧州渤海新区绿色化工研究院,沧州061100 [4]天津国际生物医药联合研究院,天津300457

出　　处：《化学通报》2021年第9期952-957,共6页Chemistry

基　　金：南开大学沧州渤海新区绿色化工研究院基金项目(NCC2020FH01)资助。

摘　　要：布帕伐醌是一种治疗牛泰勒焦虫病的药物,其传统的合成工艺存在产率低、污染严重以及成本过高的问题。本文在目前布帕伐醌的合成工艺上进行了优化,以1,4-萘醌作为起始原料,经过4步转化合成得到布帕伐醌,反应总收率达到62%,产品纯度可达99%以上,该方法在布帕伐醌的大规模生产上具有很好的应用前景。Buparvone is an effective veterinary drug for the treatment of bovine theileriosis which is a kind of dangerous blood-borne disease to cattle. However the large scale synthesis of Buparvone is still challenging, the overall yield is low and the cost is too high, especially that its environmental pollution is still a problem. In this article, we reported an improved synthetic method of Buparvone with high yield and simple operation using 1,4-naphthoquinone as the starting material. The total yield could reach to 62% for 4 steps and the purity of product is more than 99%. This novel method is very promising in further large scale production of Buparvone.

关 键 词：布帕伐醌 泰勒焦虫病 改进合成方法 

分 类 号：S859.53[农业科学—临床兽医学]