Chin. J. Org. Chem. ›› 2013, Vol. 33 ›› Issue (07): 1564-1567.DOI: 10.6023/cjoc201301038 Previous Articles     Next Articles

Notes

康布瑞汀磷酸酯二钠盐合成工艺的优化

肖繁花, 吴范宏   

  1. 上海应用技术学院化学与环境工程学院 上海 201418
  • 收稿日期:2013-01-16 修回日期:2013-02-21 发布日期:2013-03-07
  • 通讯作者: 吴范宏 E-mail:wfh@sit.edu.cn

Process Optimization for the Synthesis of Disodium Combretastatin A-4 Phosphate

Xiao Fanhua, Wu Fanhong   

  1. School of Chemical and Environmental Engineering, Shanghai Institute of Technology, Shanghai 201418
  • Received:2013-01-16 Revised:2013-02-21 Published:2013-03-07

The method for the synthesis of disodium combretastatin A-4 phosphate was studied. The target product was prepared from 3,4,5-trimethoxyl benzaldehyde as the starting material, through 7-step reactions including reduction, bromation, phosphonium salt formation, Wittig reaction, detritylation reaction, dibenzylphosphorylation reaction, deprotection and disodium salt formation. Disodium combretastaton A-4 phosphate (1) was prepared with HPLC purity of 99. 8% and the total yield of 43.0%. The optimized synthetic process has the advantages of available starting material, simplicity and cheapness, which was more suitable for industrialized production.

Key words: disodium combretastatin A-4 phosphate, anti-cancer drug, synthesis