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›› 2006, Vol. 6 ›› Issue (1): 91-95.

• 生化工程专栏 • 上一篇    下一篇

20(S)-9-硝基喜树碱的合成

白云峰,贾梦秋,安辉,徐春艳   

  1. 北京化工大学材料科学与工程学院
  • 出版日期:2006-02-20 发布日期:2006-02-20

Synthesis of 20(S)-9-Nitro-camptothecin

BAI Yun-Feng,JIA Meng-Qiu,AN Hui,XU Chun-Yan   

  1. College of Materials Science and Engineering，Beijing University of Chemical Technology
  • Online:2006-02-20 Published:2006-02-20

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被引次数

1

摘要： 介绍了一种以无机硝酸盐为硝化剂、喜树碱为原料、浓硫酸为溶剂合成9-硝基喜树碱(9-NC)的新方法. 在此硝化反应体系中，合成9-NC的最佳工艺条件为喜树碱0.5 g，浓硫酸40 mL, ?NO3- 0.007 mol, KNO3/Sr(NO3)2为1:1. 在冰盐浴下反应4 h，再于40℃下反应1 d得到9-NC初产物，经柱层析后，产品收率为41.1%，9-NC纯度98.8%(w)，均高于文献值.

关键词: 喜树碱, 9-硝基喜树碱, 硝化反应, 合成

Abstract: A new method for synthesizing 20(S)-9-Nitro-camptothecin was proposed by using inorganic nitrates as nitration reagents, camptothecin as the raw material, and concentrated sulfuric acid as solvent. The best reaction conditions were: camptothecin 0.5 g, concentrated sulfuric acid 40 mL, ?NO3- 0.007 mol, and KNO3/Sr(NO3)2 1:1 (molar ratio). The nitration procedure was carried out in ice-salt bath for 4 h and then at 40℃ for 1 d. The crude nitration products were purified by column chromatography. The total yield of nitration products was 41.1% (40% in the literature) with 98.8% (98% in the literature) purity for 9-NC.

Key words: camptothecin, 9-nitro-camptothecin, nitration, synthesis