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Chinese Journal of Organic Chemistry >

2013 , Vol. 33 >Issue 07: 1564 - 1567

DOI: https://doi.org/10.6023/cjoc201301038

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

  • Xiao Fanhua ,
  • Wu Fanhong
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  • School of Chemical and Environmental Engineering, Shanghai Institute of Technology, Shanghai 201418

Received date: 2013-01-16

  Revised date: 2013-02-21

  Online published: 2013-03-07

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Abstract

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

Cite this article

Xiao Fanhua , Wu Fanhong . Process Optimization for the Synthesis of Disodium Combretastatin A-4 Phosphate[J]. Chinese Journal of Organic Chemistry, 2013 , 33(07) : 1564 -1567 . DOI: 10.6023/cjoc201301038

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