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盐酸表柔比星的合成

摘要:盐酸多柔比星经氨基三氟乙酰化、双羟基保护、与三氟甲磺酸酐成酯、与三乙胺甲酸盐进行亲核取代反应、水解

酯和酰胺、脱双羟基保护、NM100大孔吸附树脂柱色谱纯化等一系列操作制得盐酸表柔比星,总收率50%。

关键词:盐酸表柔比星盐酸多柔比星;蒽环类抗肿瘤抗生素;合成


ABSTRACT:  Epirubicin  hydrochloride  was  synthesized  from  doxorubicin  hydrochloride  through  trifluoroacetylation, bishydroxy protection, esterification with trifluoromethanesulfonic anhydride, substitution with triethylamine 

formate, hydrolysis of ester and amide, bishydroxy deprotection, and purification with macroporou resin NM100 column  chromatography. The overall yield was 50 %.

Key Words : epirubicin hydrochloride; doxorubicin hydrochloride; anthracycline antitumor antibiotics; synthesis

















   本文收录于"中国医药工业杂志  Chinese Journal of  Pharmaceuticals 2016,  47(5)"


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