研究简报

汉黄芩素的方便合成

  • 董玮 ,
  • 王欣 ,
  • 葛泽梅 ,
  • 和芳 ,
  • 李润涛
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  • a 北京大学药学院 天然药物及仿生药物国家重点实验室 北京 100191;
    b 北京创立科创医药技术开发有限公司 北京 100029

收稿日期: 2020-01-29

  修回日期: 2020-03-17

  网络出版日期: 2020-04-10

基金资助

国家自然科学基金(No.81673287)资助项目.

Efficient Synthesis of Wogonin

  • Dong Wei ,
  • Wang Xin ,
  • Ge Zemei ,
  • He Fang ,
  • Li Runtao
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  • a State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191;
    b Beijing Supertrack Pharma-Tech Co., LTD, Beijing 100029

Received date: 2020-01-29

  Revised date: 2020-03-17

  Online published: 2020-04-10

Supported by

Project supported by the National Natural Science Foundation of China (No. 81673287).

摘要

汉黄芩素(Wogonin)是一种重要的黄酮类化合物,具有广泛的药理活性,其研究越来越受到重视.汉黄芩素的大量获得是对其深入研究的基础,但目前存在从天然产物中提取困难、全合成原料不易获得、反应条件苛刻、贵重及有毒试剂的使用、分离纯化困难或收率低等问题.以间苯三酚为原料,经七步反应得到汉黄芩素,总收率达到58%.具有原料及试剂便宜易得、反应条件温和、操作简便及无需柱层析纯化等优点,为汉黄芩素的规模化制备及深入研究奠定了基础.

本文引用格式

董玮 , 王欣 , 葛泽梅 , 和芳 , 李润涛 . 汉黄芩素的方便合成[J]. 有机化学, 2020 , 40(6) : 1725 -1730 . DOI: 10.6023/cjoc202001033

Abstract

Wogonin is an important flavonoid with a wide range of pharmacological activities, and its research has received increasing attention. The large amount of wogonin is the basis of in-depth research on it, but currently there are problems, such as difficulty in extracting from natural products, difficult to obtain fully synthetic raw materials, harsh reaction conditions, use of valuable and toxic reagents, difficulty in isolation and purification, or low yields. Herein, an efficient synthesis of wogonin from benzene-1,3,5-triol as starting material via seven steps with total yield of 58% was reported. This method possesses advantages including available starting materials, mild reaction conditions, simple operation and no column chromatography purification, which will provide a foundation for the large-scale preparation and in-depth study of wogonin.

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