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有机化学 ›› 2008, Vol. 28 ›› Issue (07): 1243-1246. 上一篇    下一篇

研究简报

一种4β-氨基鬼臼毒素的合成新方法

徐 晖*,a ; 张 雷a ; 田 瑄b   

  1. (a西北农林科技大学理学院药物合成实验室 杨凌 712100)
    (b兰州大学化学系应用有机化学国家重点实验室 兰州 730000)
  • 收稿日期:2007-10-29 修回日期:2007-12-28 发布日期:2008-07-28
  • 通讯作者: 徐 晖

A Highly Improved Synthesis of 4β-Aminopodophyllotoxin

XU, Hui*,a ZHANG, Leia TIAN, Xuanb   

  1. (a Laboratory of Pharmaceutical Synthesis, College of Sciences, Northwest Agriculture & Forestry University,
    Yangling 712100)
    (b State Key Laboratory of Applied Organic Chemistry, Department of Chemistry, Lanzhou University, Lanzhou 730000)
  • Received:2007-10-29 Revised:2007-12-28 Published:2008-07-28
  • Contact: XU, Hui

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649

被引次数

7 | 2

报道了一种在室温条件下和在四氢呋喃水溶液中用Zn/HCO2NH4还原4β-叠氮鬼臼毒素制备抗癌药物中间体4β-氨基鬼臼毒素的新方法. 此方法具有产率高(96%)、不需要用贵金属(如钯或钐)催化和无水条件、操作方便等优点. 最佳的反应条件为: 底物、Zn和HCO2NH4的物质的量之比为1∶2∶4, 反应溶剂为85%四氢呋喃水溶液, 反应时间为5 h.

关键词: 4β-氨基鬼臼毒素, 合成, 4β-叠氮鬼臼毒素, 抗癌, 还原

4β-Aminopodophyllotoxin, a very important intermediate of anticancer drugs, has been successfully synthesized from 4β-azidopodophyllotoxin in a 96% yield by reduction with Zn/HCO2NH4 in 85% aq. tetrahydrofuran for 5 h. Compared to the reported results, advantages of this method are as follows: very ex-cellent yield, no need for any anhydrous conditions, use of inexpensive metals, and very convenient, practi-cal and simple procedure.

Key words: 4β-azidopodophyllotoxin, synthesis, reduction, anticancer, 4β-aminopodophyllotoxin