- 专利标题: Processes for preparing 6-hydroxy-3,4-dihydroquinolinone, cilostazol and N-(4-methoxyphenyl)3-chloropropionamide
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申请号: US10094050申请日: 2002-03-08
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公开(公告)号: US06660773B2公开(公告)日: 2003-12-09
- 发明人: Marioara Mendelovici , Gideon Pilarsky , Tamar Nidam , Ben-Zion Dolitzky
- 申请人: Marioara Mendelovici , Gideon Pilarsky , Tamar Nidam , Ben-Zion Dolitzky
- 主分类号: C07C20910
- IPC分类号: C07C20910
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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