袁昊林,赵彦梁,范东升,杨阳,贺万丽,赵佩佩,蔡岩.化学通报,2021,84(9):952-957.
布帕伐醌的改进合成方法
An Improved Synthetic Method of Buparavone
投稿时间:2021-02-04  修订日期:2021-02-17
DOI:
中文关键词:  布帕伐醌  泰勒焦虫病  改进合成方法
英文关键词:Buparvone  Bovine theileriosis  Improved synthetic method
基金项目:南开大学沧州渤海新区绿色化工研究院基金项目(NCC2020FH01)资助
作者单位E-mail
袁昊林  zhaopp_89@163.com 
赵彦梁 喀什大学化学与环境科学学院  
范东升 喀什大学化学与环境科学学院  
杨阳 南开大学药学院  
贺万丽 天津国际生物医药联合研究院  
赵佩佩 天津国际生物医药联合研究院 天津 南开大学药学院 天津  
蔡岩* 天津国际生物医药联合研究院 caiyan_86@163.com 
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中文摘要:
      布帕伐醌是一种治疗牛泰勒焦虫病的药物,布帕伐醌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,该方法以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
英文摘要:
      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 total yield is still unsatisfactory and the cost is still 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, we used 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.
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