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红霉素肟的合成研究
引用本文:潘 冰,杨英梅.红霉素肟的合成研究[J].河北工业科技,2009,26(4):237-239.
作者姓名:潘 冰  杨英梅
作者单位:石药集团欧意药业有限公司一车间,河北石家庄,050051
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。

关 键 词:硫氰酸红霉素  红霉素肟  合成  工艺改进
收稿时间:2009/4/2 0:00:00
修稿时间:2009/5/15 0:00:00

Study on synthesis of erythromycin oxime
PAN Bing and YANG Ying-mei.Study on synthesis of erythromycin oxime[J].Hebei Journal of Industrial Science & Technology,2009,26(4):237-239.
Authors:PAN Bing and YANG Ying-mei
Institution:No.1Workshop,Ouyi Pharmaceutical Company Limited,CSPC,Shijiazhuang Hebei 050051,China;No.1Workshop,Ouyi Pharmaceutical Company Limited,CSPC,Shijiazhuang Hebei 050051,China
Abstract: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.
Keywords:erythromycin thiocyanate  erythromycin oxime  synthesis  process improvement
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