天然产物研究与开发 ›› 2016, Vol. 28 ›› Issue (增刊2): 244-246.doi: 10.16333/j.10016880.2016.S.012

• 研究论文 • 上一篇    下一篇

10羟基喜树碱及其衍生物的合成

戴汉松*,骆贵文,邓龙,罗虹,刘正立   

  1. 四川师范大学化学与材料科学学院,成都 610068
  • 出版日期:2016-12-31 发布日期:2017-03-03

Synthesis of 10Hydroxycamptothecin and Its New Derivatives

DAI Hansong*,LUO Guiwen,DENG Long,LUO Hong,LIU Zhengli   

  1. Department of Chemistry and Materials Science,Sichuan Normal University,Chengdu 610068,China
  • Online:2016-12-31 Published:2017-03-03

摘要: 本论文研究了以喜树碱为原料,经光照法等合成10羟基喜树碱,再用自制的N乙氧羰基S脯氨酸与10羟基喜树碱反应,合成了其新衍生物10脯氨酸喜树碱,对其结构用1H NMR进行了表征。结果表明,10羟基喜树碱产率为63%;得到了10脯氨酸喜树碱,产率为53.8%。新合成物中的脯氨酸和喜树碱在抗肿瘤治疗中可能起到一定的协同效应。

关键词: 合成, 10羟基喜树碱, 抗肿瘤活性, 10脯氨酸喜树碱

Abstract: This essay studied with camptothecin as raw materials,synthesized 10hydroxy camptothecin by illumination method,and then has obtained N ethoxycarbonyl S proline is reacted with HCPT synthesized its new derivatives 10 prolinecamptothecin,its structure was characterized by 1HNMR. The results showed that HCPT 63% yield,10 prolinecamptothecin's is 53.8%. The new composition of the proline and camptothecin anticancer therapy may play a synergistic effect.

Key words: synthesis, 10hydroxycamptothecin, antitumor activity, 10prolinecamptothecin

中图分类号: 

R73