盐酸表柔比星的合成  

Synthesis of Epirubicin Hydrochloride

作　　者：贾淼[1] 裘鹏程[1] 焦慧荣 汪有贵 张福利[1] 

机构地区：[1]中国医药工业研究总院上海医药工业研究院,创新药物与制药工艺国家重点实验室,上海200437 [2]浙江海正药业股份有限公司,浙江台州318000

出　　处：《中国医药工业杂志》2016年第5期522-527,共6页Chinese Journal of Pharmaceuticals

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%。Epirubicin hydrochloride was synthesized from doxorubicin hydrochloride through trifluoro- acetylation, 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 %.

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 

分 类 号：R979.14[医药卫生—药品]