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Improved synthesis of Etimiein sulfate
Author(s): 
Pages: 106-108
Year: Issue:  2
Journal: QILU PHARMACEUTICAL AFFAIRS

Keyword:  硫酸依替米星1-N-乙基庆大霉素C1a过渡金属络合物硅烷化N-乙基化;
Abstract: 目的改进硫酸依替米星的合成工艺.方法以庆大霉素C1a为起始原料,采用过渡金属络合物催化方法保护部分氨基,并应用了发明专利未曾报道的硅烷化羟基保护新步骤,用缩合-还原型N-乙基化反应得到了1-N-乙基庆大霉素C1a,与硫酸成盐合成了符合国家药品质量标准的硫酸依替米星原料药成品.结果收率为37.3%,较发明专利有明显的提高,本工艺中试也取得了较好的结果.结论该改进工艺具有一定的产业化价值.
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