Chin. J. Org. Chem. ›› 2010, Vol. 30 ›› Issue (9): 1335-1341. Previous Articles     Next Articles

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微波辐射下6-烷氧基大黄酸的合成及抑菌活性研究

朱小康1,叶小利2,袁吕江1,朱家颖1,丁阳平1,李学刚*,1   

  1. (1西南大学药学院 重庆 400716)
    (2西南大学生命科学院 重庆 400716)
  • 收稿日期:2009-10-23 修回日期:2010-02-02 发布日期:2010-04-21
  • 通讯作者: 朱小康 E-mail:xiaokangzhu1982@yahoo.com.cn
  • 基金资助:

    国家级.国家自然科学基金

Microwave-Assisted Synthesis and Antibacterial Activity of 6-Alkoxy Rheins

Zhu Xiaokang1 Ye Xiaoli2 Yuan Luji-ang1 Zhu Jiaying1 Ding Yangping1 Li Xuegang*,1   

  1. (1 School of Pharmaceutical Science, Southwest University, Chongqing 400716)
    (2 School of Life Science, Southwest University, Chongqing 400716)
  • Received:2009-10-23 Revised:2010-02-02 Published:2010-04-21
  • Contact: ZHU Xiao-Ming E-mail:xiaokangzhu1982@yahoo.com.cn

Five new 6-alkoxy rheins have been designed and synthesized through Williamson reaction, acetyl protection, oxidation reaction and deprotection. The effects of microwave and conventional method on the yield of 3-alkyl emodin derivatives were compared. The effects of different oxidants in the synthesis of 3a3e were studied and the best oxidation conditions were found. All the structures have been confirmed by IR, 1H NMR, MS and HRMS techniques. The minimal inhibitory concentration (MIC) assay indicated that antibacterial activity changes regularly, as the alkyl chain growth.

Key words: emodin, 6-alkoxy rhein, microwave, oxidation, antibacterial activity