康布瑞汀磷酸酯二钠盐合成工艺的优化

doi:10.6023/cjoc201301038

摘要/Abstract

本文对康布瑞汀磷酸酯二钠盐的合成工艺进行优化。确定了以3, 4, 5-三甲氧基苯甲醛为原料, 经还原、溴代、成鏻盐合成中间体3, 4, 5-三甲氧基苄溴三苯基鏻盐;鏻盐与3-三苯甲氧基-4-甲氧基苯甲醛经Wittig反应、脱三苯甲基保护基、与亚磷酸二苄酯成酯、脱苄基成钠盐得到康布瑞汀磷酸酯二钠盐的方法。所得康布瑞汀磷酸酯二钠盐(1), HPLC纯度达99.5%。总收率为43.0%。经优化后的工艺原料价廉易得, 操作简便, 成本低廉, 适合于工业化生产。

关键词: 康布瑞汀磷酸酯二钠, 抗癌药, 合成

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

引用此文

肖繁花, 吴范宏. 康布瑞汀磷酸酯二钠盐合成工艺的优化[J]. 有机化学, 0, (0): 0-0.

XIAO Fan-hua, WU Fan-hong. The process optimization for the synthesis of disodium Combretastatin A-4 phosphate[J]. Chin. J. Org. Chem., 0, (0): 0-0.

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