The process optimization for the synthesis of disodium Combretastatin A-4 phosphate
Online 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.
XIAO Fan-hua , WU Fan-hong . The process optimization for the synthesis of disodium Combretastatin A-4 phosphate[J]. Chinese Journal of Organic Chemistry, 0 , (0) : 0 -0 . DOI: 10.6023/cjoc201301038
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