有机化学 ›› 2012, Vol. 32 ›› Issue (12): 2378-2381.DOI: 10.6023/cjoc201205025 上一篇    下一篇

研究简报

微波技术在10-羟基喜树碱醚化反应中的应用

孟光荣a, 李嘉俊a, 张倩a, 马红梅b   

  1. a 复旦大学药学院药物化学教研室 上海 201203;
    b 华东理工大学药学院 上海 200237
  • 收稿日期:2012-05-19 修回日期:2012-08-01 发布日期:2012-08-10
  • 通讯作者: 马红梅 E-mail:hmma@ecust.edu.cn
  • 基金资助:
    创新药物平台(No. 2009ZX09301-011)资助项目.

Application of Microwave Technique into Etherification of 10-Hydroxycamptothecin

Meng Guangronga, Li Jiajuna, Zhang Qiana, Ma Hongmeib   

  1. a Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 201203;
    b School of Pharmacy, East China University of Science & Technology, Shanghai 200237
  • Received:2012-05-19 Revised:2012-08-01 Published:2012-08-10
  • Supported by:
    Project supported by the National Drug Innovative Program (No. 2009ZX09301-011).

为减少喜树碱结构在碱性条件下的内酯环开环反应, 将微波技术应用于10-羟基喜树碱的醚化反应中, 与常规加热条件相比, 微波反应不仅极大地缩短了反应时间, 同时也将反应收率从20%~30%显著地提高到50%~83%. 这一研究结果对喜树碱的其他类型反应也具有可借鉴作用.

关键词: 10-羟基喜树碱, 醚化反应, 微波技术

In an effort to reduce the cleavage of E lactone ring in camptothecin, microwave technique was applied in the etherification of 10-hydroxycamptothecin. Compared with the conventional heating condition, microwave can truncate the reaction time and improve the yield from 20%~30% to 50%~83% significantly. Furthermore, this reaction condition could be used for reference in other relative reactions of camptothecins.

Key words: 10-hydroxycamptothecin, etherification, microwave technology