发明名称 |
Processes for preparing 6-hydroxy-3,4-dihydroquinolinone, cilostazol and N-(4-methoxyphenyl)3-chloropropionamide |
摘要 |
A process for preparing 6-hydroxy-3,4-dihydroquinolinone by intramolecular Friedel-Crafts alkylation of N-(4-methoxyphenyl)-3-chloropropionamide in which an equivalent of N-(4-methoxyphenyl)-3-chloropropionamide is contacted with a Lewis acid in DMSO or a high boiling amide or amine at an elevated temperature of from about 150° C. to about 220° C. is provided. The process produces 6-HQ in high yield and a high state of purity such that it may be used in subsequent reactions toward the preparation of cilostazol without intermediate purification. A process for preparing cilostazol from 6-hydroxy-3,4-dihydroquinolinone prepared by the process and improved processes for preparing N-(4-methoxyphenyl)-3-chloropropionamide are also provided.
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申请公布号 |
US6660773(B2) |
申请公布日期 |
2003.12.09 |
申请号 |
US20020094050 |
申请日期 |
2002.03.08 |
申请人 |
TEVA PHARMACEUTICAL INDUSTRIES, LTD. |
发明人 |
MENDELOVICI MARIOARA;PILARSKY GIDEON;NIDAM TAMAR;DOLITZKY BEN-ZION |
分类号 |
C07C231/02;C07C233/25;C07D215/22;C07D215/227;(IPC1-7):C07C209/10;A61K31/167 |
主分类号 |
C07C231/02 |
代理机构 |
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