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    Processes for preparing 6-hydroxy-3,4-dihydroquinolinone, cilostazol and N-(4-methoxyphenyl)-3-chloropropionamide
    3.
    发明授权
    Processes for preparing 6-hydroxy-3,4-dihydroquinolinone, cilostazol and N-(4-methoxyphenyl)-3-chloropropionamide 失效
    制备6-羟基-3,4-二氢喹啉酮，西洛他唑和N-（4-甲氧基苯基）-3-氯丙酰胺的方法

    公开(公告)号：US06967209B2

    公开(公告)日：2005-11-22

    申请号：US10372201

    申请日：2003-02-25

    申请人： Marioara Mendelovici ,  Gideon Pilarsky ,  Tamar Nidam ,  Ben-Zion Dolitzky

    发明人： Marioara Mendelovici ,  Gideon Pilarsky ,  Tamar Nidam ,  Ben-Zion Dolitzky

    IPC分类号： C07C231/02 ,  C07C233/25 ,  C07D215/22 ,  C07D215/227 ,  A61K31/4704

    CPC分类号： C07D215/227 ,  C07C231/02 ,  C07C233/25

    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.

    摘要翻译： 通过N-（4-甲氧基苯基）-3-氯丙酰胺的分子内Friedel-Crafts烷基化制备6-羟基-3,4-二氢喹啉酮的方法，其中将当量N-（4-甲氧基苯基）-3-氯丙酰胺与 提供了在约150℃至约220℃的高温下在DMSO中的路易斯酸或高沸点酰胺或胺。 该方法以高产率和高纯度产生6-HQ，使得其可用于随后的用于西洛他唑制备的反应，而无需中间纯化。 还提供了通过该方法制备西洛他唑的方法和改进的制备N-（4-甲氧基苯基）-3-氯丙酰胺的方法。

    Processes for preparing 6-hydroxy-3,4-dihydroquinolinone, cilostazol and N-(4-methoxyphenyl)-3-chloropropionamide
    5.
    发明授权
    Processes for preparing 6-hydroxy-3,4-dihydroquinolinone, cilostazol and N-(4-methoxyphenyl)-3-chloropropionamide 失效
    制备6-羟基-3,4-二氢喹啉酮，西洛他唑和N-（4-甲氧基苯基）-3-氯丙酰胺的方法

    公开(公告)号：US06740758B2

    公开(公告)日：2004-05-25

    申请号：US10465885

    申请日：2003-06-20

    申请人： Marioara Mendelovici ,  Gideon Pilarsky ,  Tamar Nidam ,  Ben-Zion Dolitzky

    发明人： Marioara Mendelovici ,  Gideon Pilarsky ,  Tamar Nidam ,  Ben-Zion Dolitzky

    IPC分类号： C07D21536

    CPC分类号： C07D215/227 ,  C07C231/02 ,  C07C233/25

    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-methoxphenyl)-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.

    摘要翻译： 通过N-（4-甲氧基苯基）-3-氯丙酰胺的分子内Friedel-Crafts烷基化制备6-羟基-3,4-二氢喹啉酮的方法，其中将当量N-（4-甲氧基苯基）-3-氯丙酰胺与 提供了在约150℃至约220℃的高温下在DMSO中的路易斯酸或高沸点酰胺或胺。 该方法以高产率和高纯度产生6-HQ，使得其可用于随后的用于西洛他唑制备的反应，而无需中间纯化。 还提供了通过该方法制备西洛他唑的方法和改进的制备N-（4-甲氧基苯基）-3-氯丙酰胺的方法。