发明名称 |
METHOD OF PREPARING CLARITHROMYCIN OF FORM II CRYSTALS |
摘要 |
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.
|
申请公布号 |
CA2402201(C) |
申请公布日期 |
2007.06.05 |
申请号 |
CA20012402201 |
申请日期 |
2001.03.14 |
申请人 |
HANMI PHARM. CO., LTD. |
发明人 |
YUN, SANG MIN;SEONG, MI RA;KIM, GI JEONG;LEE, GWAN SUN;SUH, KWEE HYUN;KIM, NAM DU |
分类号 |
C07H17/08;A61K31/7048;A61P1/04;A61P31/04 |
主分类号 |
C07H17/08 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|