Chin. J. Org. Chem. ›› 0, Vol. ›› Issue (0): 0-0.DOI: 10.6023/cjoc201301038    



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
  • 出版日期:2013-12-31 发布日期:2013-03-07
  • 通讯作者: 肖繁花

The process optimization for the synthesis of disodium Combretastatin A-4 phosphate

XIAO Fan-hua, WU Fan-hong   

  1. School of Chemica and Environmental Engineering, Shanghai Institute of Technology,Shanghai 200235, China
  • Online:2013-12-31 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 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