中华医学超声杂志

应用化学 ›› 2010, Vol. 27 ›› Issue (09): 1038-1041.DOI: 10.3724/SP.J.1095.2010.90715

• 研究论文 • 上一篇    下一篇

黄芩素A环的结构修饰

祝正辉1,2,雷泽3,蒋明忠4,木晓云3,付正启3,温晓江3,朱洪友1,3*   

  1. (1.云南大学化学科学与工程学院,教育部自然资源药物化学重点实验室 昆明 650091;2.益阳市环境监测站 益阳;
    3.昆明云大医药开发有限公司 昆明 650222;4.云南警官学院 昆明)
  • 收稿日期:2009-10-30 修回日期:2010-02-25 出版日期:2010-09-10 发布日期:2010-09-10
  • 通讯作者: 朱洪友，男，教授; E-mail:hongyouzhu@Sohu.com; 研究方向：有机合成
  • 基金资助:
    云南省自然科学基金（2003C009M）资助项目

Structural Modification of the A-ring Baicalein

ZHU Zheng-Hui1,2, LEI Ze3, JIANG Ming-Zhong4, MU Xiao-Yun3, FU Zheng-Qi3, WEN Xiao-Jiang3, ZHU Hong-You1,3*   

  1. (1.Chemical Science and Engineering College of Yunnan University,Key Laboratory of Medicinal
    Chemistry for Natural Resource of Ministry of Education,Yunnan University,Kunming 650091;
    2.Yiyang Enviromental Monitoring Station,Yiyang;
    3.Yunnan University Medical Development Co.,Ltd,Kunming 650222;
    4.Yunnan Police Officer Academy,Kunming)
  • Received:2009-10-30 Revised:2010-02-25 Published:2010-09-10 Online:2010-09-10

PDF

1216

被引次数

4

摘要：

以传统中药黄芩的主要活性成分黄芩苷及其乙酰化产物6,7-二乙酰氧基黄芩素为原料，通过碘代、硝化及硝基还原胺化反应在A环的C-8上引入碘原子、硝基及胺基，并对黄芩素A环上的3个酚羟基进行了选择性二甲醚化及全甲醚化，制备了A环修饰的6种黄芩素衍生物，表征了它们的结构，讨论了合成方法的特点。

关键词: 黄芩苷, 二乙酰氧基黄芩素, 选择性甲醚化, 结构修饰

Abstract:

Using baicalin, the main active component of a traditional Chinese herb Scutellaria baicalensis, and one of its derivative, 6,7-diacetoxylbaicalein, as precursors, a series of C8-substituted and di or tri-O-methylated baicalein derivatives was synthesized in good yields by iodination, nitration, reductive amination and selective methoxylation or hydrolysis of 6,7-diacetoxylbaicalein. The structures of these producrs were characterized. They featured with a broad spectrum of biological activities, notably anti-oxidant.

Key words: baicalin, diacetoxylbaicalein, selective methoxylation, structural modification

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