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有机化学
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有机化学 ›› 2008, Vol. 28 ›› Issue (11): 1982-1985. 上一篇    下一篇

研究简报

5,7-二甲氧基-4-甲基苯酞和5,7-二羟基-4-甲基苯酞的新合成方法

左 理; 姚珊燕; 段文虎*   

  1. (中国科学院上海生命科学研究院上海药物研究所 上海 201203)
  • 收稿日期:2008-03-07 修回日期:2008-05-14 发布日期:2008-11-18
  • 通讯作者: 段文虎

New Synthetic Methods of 5,7-Dimethoxy-4-methylphthalide and 5,7-Dihydroxy-4-methylphthalide

ZUO, Li ; YAO, Shan-Yan; DUAN, Wen-Hu*   

  1. (Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences,
    Chinese Academy of Sciences, Shanghai 201203)
  • Received:2008-03-07 Revised:2008-05-14 Published:2008-11-18
  • Contact: DUAN, Wen-Hu

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被引次数

1

以3,5-二甲氧基苯甲醇为起始原料, 经过五步反应, 合成了5,7-二甲氧基-4-甲基苯酞和5,7-二羟基-4-甲基苯酞这两个用于合成霉酚酸的重要中间体, 产率分别达到80%和72%. 6-氯甲基-2,4-二甲氧基苯甲醛经过亚氯酸钠氧化成酸的同时发生内酯化反应生成5,7-二甲氧基苯酞是最关键的一步.

关键词: 5,7-二羟基-4-甲基苯酞, 霉酚酸, 合成, 5,7-二甲氧基-4-甲基苯酞

5,7-Dimethoxy-4-methylphthalide and 5,7-dihydroxy-4-methylphthalide, two key intermediates in the synthesis of mycophenolic acid, were prepared from 3,5-dimethoxybenzyl alcohol in a five-step sequence with yields of 80% and 72%, respectively. The key process involved a transformation of 6-chloromethyl-2,4-dimethoxybenzaldehyde to 5,7-dimethoxyphthalide by an oxidation with sodium chlo-rite and a concomitant lactonization in one pot.

Key words: 5,7-dihydroxy-4-methylphthalide, mycophenolic acid, synthesis, 5,7-dimethoxy-4-methylphthalide