发明名称 |
Method of preparing form II crystals of clarithromycin |
摘要 |
High purity Form II crystals of clarithromycin 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.
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申请公布号 |
US6515116(B2) |
申请公布日期 |
2003.02.04 |
申请号 |
US20010805831 |
申请日期 |
2001.03.14 |
申请人 |
HANMI PHARM. CO., |
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;C07H1/00 |
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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