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    Processes for preparing 6-hydroxy-3,4-dihydroquinolinone, cilostazol and N-(4-methoxyphenyl)-3-chloropropionamide
    4.
    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。

    Method for preparing benzisoxazole methane sulfonyl chloride and its amidation to form zonisamide
    6.
    发明授权
    Method for preparing benzisoxazole methane sulfonyl chloride and its amidation to form zonisamide 失效
    制备苯并异恶唑甲磺酰氯及其酰胺化形成唑尼沙胺的方法

    公开(公告)号：US06936720B2

    公开(公告)日：2005-08-30

    申请号：US10373554

    申请日：2003-02-24

    申请人： Marioara Mendelovici ,  Neomi Gershon ,  Tamar Nidam ,  Gideon Pilarski ,  Greta Sterinbaum

    发明人： Marioara Mendelovici ,  Neomi Gershon ,  Tamar Nidam ,  Gideon Pilarski ,  Greta Sterinbaum

    IPC分类号： A61K31/423 ,  A61P25/08 ,  C07B61/00 ,  C07D261/20 ,  C07D405/12

    CPC分类号： C07D261/20 ,  C07D405/12

    摘要： The present invention relates to a process of preparing benzisoxazole methane sulfonic acid-chloride (BOS—Cl) as an zonisamide intermediate via chlorination of benzisoxazole methane sulfonate. The present invention also discloses a process of preparing zonisamide via amidation of BOS—Cl. More particularly, the present invention provides a process of preparing zonisamide, comprising the steps of: a) chlorinating BOS, salts or esters thereof, with SOCl2 in an organic solvent and/or in the presence of a catalyst to form BOS—Cl; and b) amidating BOS—Cl in the presence of ammonia selected from the group consisting of aqueous ammonia in a biphasic system, masked ammonia and dry ammonia to form zonisamide.

    摘要翻译： 本发明涉及通过苯并异恶唑甲烷磺酸盐的氯化制备苯并异恶唑甲磺酸氯化物（BOS-Cl）作为唑烷酰胺中间体的方法。 本发明还公开了通过BOS-Cl的酰胺化制备唑尼沙胺的方法。 更具体地说，本发明提供了制备唑尼沙胺的方法，包括以下步骤：a）在有机溶剂中和/或在有机溶剂存在下，将BOS，其盐或酯与SOCl 2氯化， 催化剂形成BOS-Cl; 和b）在选自二元体系中的氨水，掩蔽的氨和干氨中的氨存在下使BOS-Cl酰胺化以形成唑尼沙胺。

    Processes for preparing 6-hydroxy-3,4-dihydroquinolinone, cilostazol and N-(4-methoxyphenyl)-3-chloropropionamide
    8.
    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。