| 罗红霉素合成过程的杂质控制 |
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| 引用本文： | 连苗利,金勇,王兆刚,张兴东,侯仲轲,邱家军.罗红霉素合成过程的杂质控制[J].精细化工中间体,2010,40(2):44-47. |
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| 作者姓名： | 连苗利 金勇 王兆刚 张兴东 侯仲轲 邱家军 |
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| 作者单位： | 浙江国邦药业有限公司,浙江,上虞,312369 |
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| 摘 要： | 红霉素A硫氰酸盐与盐酸羟胺缩合成红霉素A-9-肟,红霉素肟与甲氧乙氧氯甲醚反应生成罗红霉素。研究了反应温度、反应时间以及物料配比对罗红霉素合成过程中杂质产生的影响,得到较优反应条件:n(红霉素肟):n(甲醇钠):n(甲氧基乙氧基氯甲醚)=1:1.12:1.21,甲醇钠和甲氧基乙氧基氯甲醚(MEMCl)的滴加时间分别为15min、45min;滴加甲醇钠时控制温度为5℃、滴加MEMCl的温度为0℃。此时的收率为95.8%(n/n)。
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| 关 键 词： | 抗生素 罗红霉素 合成 |
Impurities Control in the Synthesis of Roxithromycin |
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| LIAN Miao-li,JIN Yong,WANG Zhao-gang,ZHANG Xing-dong,HOU Zhong-ke,QIU Jia-jun.Impurities Control in the Synthesis of Roxithromycin[J].Fine Chemical Intermediates,2010,40(2):44-47. |
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| Authors: | LIAN Miao-li JIN Yong WANG Zhao-gang ZHANG Xing-dong HOU Zhong-ke QIU Jia-jun |
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| Affiliation: | (Zhejiang Guobang Pharmaceutical Co., Ltd, Shangyu 312369, China) |
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| Abstract: | Reaction of thiocyanate erythromycin A with hydroxylamine hydrochloride afforded erythromycin A-9- oxime, followed by reaction with （methoxyethoxy） methyl chloride to form roxithromycin. Reaction conditions were optimized and the product was prepared in 95.8% yield. The reaction mechanism was proposed based on the analysis of by-products. |
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| Keywords: | antibiotic roxithromyein synthesis impurity |
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