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化学学报
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化学学报 ›› 2007, Vol. 65 ›› Issue (8): 711-714. 上一篇    下一篇

研究论文

加兰他敏的半合成研究

刘涛*,1, 陈新志2, 杜荣斌1, 徐国华2, 安越2   

  1. (1安庆师范学院化学化工学院 安庆 246003)
    (2浙江大学材料与化工学院 杭州 310027)
  • 投稿日期:2006-11-01 修回日期:2006-11-28 发布日期:2007-04-28
  • 通讯作者: 刘涛刘

Semi-synthesis of Galanthamine

LIU Tao*,1; CHEN Xin-Zhi2; DU Rong-Bin1; XU Guo-Hua2; AN Yue2   

  1. (1 School of Chemistry and Chemical Engineering, Anqing Normal College, Anqing 246003)
    (2 College of Materials Science and Chemical Engineering, Zhejiang Uni-versity, Hangzhou 310027)
  • Received:2006-11-01 Revised:2006-11-28 Published:2007-04-28
  • Contact: LIU Tao

PDF

1236

被引次数

31 | 3

加兰他敏提取工艺中的主要副产品——力可拉敏的药用价值明显低于加兰他敏, 为提高力可拉敏的利用价值, 在催化剂存在下脱氢制取加兰他敏. 以力可拉敏为原料, 分别考察了反应时间、温度和催化剂用量对反应的影响, 得出在9%镧镍稀土合金催化剂存在下, 240 ℃时选择性脱氢, 半合成加兰他敏, 收率达45.9%, 光学纯度为97%. 计算该反应在反应前10 min内的表观活化能为77.25 kJ/mol, 属化学反应控制过程. 产物用HPLC, IR, MS, 1H NMR和13C NMR进行定性及结构表征.

关键词: 加兰他敏, 力可拉敏, 稀土催化剂, 脱氢

In order to increase the use value of lycoramine, it was dehydrogenated selectively in the presence of 9% rare earth metal hydride at 240 ℃, affording galanthamine with 45.9% yield and 97% optical purity by semi-synthesis. The effects of reaction temperature, reaction time, and the quantity of catalyst on the re-action were examined and discussed, respectively. The value of activation energy was given to be 77.25 kJ/mol by Arrhenius equation during the former 10 min of reaction, which belongs to chemical reaction con-trol process. The resultant product of reaction was characterized by HPLC, IR, MS, 1H NMR and 13C NMR.

Key words: galanthamine, lycoramine, rare-earth catalyst, dehydrogenation