红霉素肟的合成研究  

Study on synthesis of erythromycin oxime

作　　者：潘冰[1] 杨英梅[1] 

机构地区：[1]石药集团欧意药业有限公司一车间,河北石家庄050051

出　　处：《河北工业科技》2009年第4期237-239,共3页Hebei Journal of Industrial Science and Technology

摘　　要：红霉素A9-肟是第2代新型红霉素的共同中间体。以硫氰酸红霉素为起始原料在酸-碱缓冲溶液中合成红霉素A9-肟,对其合成工艺进行了综述,对合成工艺进行了较详细的研究,开发出了一条全新的合成红霉素肟的工艺路线,使产品转化率高于90%。优化了红霉素肟合成中溶剂配比、盐酸羟胺配比、肟化反应pH值、肟化反应温度等反应条件,做了相应的稳定性实验。改进后的合成路线适合工业化生产。Erythromycin A 9-oxime is the common intermediate of the second generation erythromycin A. Erythromycin A 9-oxime is synthesized in acid-base buffer solution with the starting material erythromycin thiocyanate. In this article the synthetic routes for Erythromycin A 9-oxime were reviewed. As the result, a novel process of synthesizing erythromycin A 9-oxime line was established. The conversion rate was over 90%. In the paper, the reaction conditions for synthesis of erythromycin A 9- oxime such as solvent ratio, the ratio of hydroxylamine hydrochloride, oxime reaction pH and oxime reaction temperature were optimized. The process is more moderate and simpler.

关 键 词：硫氰酸红霉素 红霉素肟 合成 工艺改进 

分 类 号：R978.1[医药卫生—药品] TQ465.5[医药卫生—药学]