发明名称 |
Method of preparing a non-pharmaceutical grade clarithromycin |
摘要 |
<p>High purity clarithromycin of Form II crystals can be easily prepared in a high yield by a process comprising the steps of: protecting the 9-oxime hydroxy group of erythromycin A 9-oxime or a salt thereof with a tropyl group and the 2'- and 4''-hydroxy groups with trimethylsilyl groups; reacting 2',4''-O-bis(trimethylsilyl)erythromycin A 9-O-tropyloxime with a methylating agent; removing the protecting groups and the oxime group of 2',4''-O-bis(trimethylsilyl)-6-O-methylerythromycin A 9-O-tropyloxime to obtain crude clarithromycin; treating the crude clarithromycin with methanesulfonic acid in a mixture of a water-miscible organic solvent and water to obtain crystalline clarithromycin mesylate trihydrate; and neutralizing the crystalline clarithromycin mesylate trihydrate with aqueous ammonia in a mixture of a water-miscible organic solvent and water.</p> |
申请公布号 |
EP1469008(A1) |
申请公布日期 |
2004.10.20 |
申请号 |
EP20040013295 |
申请日期 |
2001.03.14 |
申请人 |
HANMI PHARM. CO., LTD. |
发明人 |
SUH, KWEE-HYUN;YUN, SANG-MIN;SEONG, MI-RA;KIM, GI-JEONG;LEE, GWAN-SUN;KIM, NAM-DU |
分类号 |
A61K31/7048;A61P1/04;A61P31/04;C07H17/08;(IPC1-7):C07H17/08 |
主分类号 |
A61K31/7048 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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