盐酸表柔比星的合成
制药工艺论坛
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)"
