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    Processes for preparing 6-hydroxy-3,4-dihydroquinolinone, cilostazol and N-(4-methoxyphenyl)-3-chloropropionamide
    1.
    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
    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：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。

    Process for the synthesis of CMHTP and intermediates thereof
    9.
    发明申请
    Process for the synthesis of CMHTP and intermediates thereof 审中-公开
    合成CMHTP的方法及其中间体

    公开(公告)号：US20080214809A1

    公开(公告)日：2008-09-04

    申请号：US12072829

    申请日：2008-02-27

    申请人： Ben-Zion Dolitzky ,  Evgeny Shapiro ,  Santiago Ini ,  Yaron Shmuely ,  Eli Lancry ,  Gideon Pilarsky

    发明人： Ben-Zion Dolitzky ,  Evgeny Shapiro ,  Santiago Ini ,  Yaron Shmuely ,  Eli Lancry ,  Gideon Pilarsky

    IPC分类号： C07D239/00

    CPC分类号： C07D471/04 ,  C07D213/73

    摘要： The present invention provides processes of preparing 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]-pyrimidin-4-one (CMHTP) useful as intermediates for the preparation of paliperidone, wherein the processes use 3-(2-chloroethyl)-2-methyl-9-benzyloxy-4H-pyrido[1,2-a]pyrimidine-4-one (CMBP) and/or 3-(2-chloroethyl)-2-methyl-9-hydroxy-4H-pyrido[1,2-a]pyrimidine-4-one (CMHP) having phosphorus at least partially removed as the intermediate.

    摘要翻译： 本发明提供制备3-（2-氯乙基）-6,7,8,9-四氢-9-羟基-2-甲基-4H-吡啶并[1,2-a]嘧啶-4-酮（ CMHTP），其用作制备利培酮的中间体，其中该方法使用3-（2-氯乙基）-2-甲基-9-苄氧基-4H-吡啶并[1,2-a]嘧啶-4-酮（CMBP）和 /或3-（2-氯乙基）-2-甲基-9-羟基-4H-吡啶并[1,2-a]嘧啶-4-酮（CMHP）作为中间体至少部分去除。

    Process for preparing 2-[(pyridinyl)methyl]sulfinyl-substituted benzimidazoles and novel chlorinated derivatives of pantoprazole
    10.
    发明授权
    Process for preparing 2-[(pyridinyl)methyl]sulfinyl-substituted benzimidazoles and novel chlorinated derivatives of pantoprazole 失效
    制备2 - [（吡啶基）甲基]亚磺酰基取代的苯并咪唑和泮托拉唑的新氯化衍生物的方法

    公开(公告)号：US07683177B2

    公开(公告)日：2010-03-23

    申请号：US10866261

    申请日：2004-06-10

    申请人： Viviana Braude ,  Nina Finkelstein ,  Kobi Chen ,  Gideon Pilarsky ,  Anita Liberman ,  Claude Singer ,  Yuriy Raizi

    发明人： Viviana Braude ,  Nina Finkelstein ,  Kobi Chen ,  Gideon Pilarsky ,  Anita Liberman ,  Claude Singer ,  Yuriy Raizi

    IPC分类号： C07D401/12

    CPC分类号： C07D401/12

    摘要： The present invention provides a process comprising admixing a thioether with about 1.05 to about 1.6 molar equivalents of an active chlorine-containing oxidant, preferably sodium hypochlorite, and about 2.5 to about 5.0 molar equivalents of an alkali metal base; and recovering a sulfoxide that is preferably pantoprazole, lansoprazole, omeprazole, or rabeprazole. The process may further comprise contacting the sulfoxide with a source of sodium ions, preferably sodium hydroxide, to produce the sodium salt of the sulfoxide. The invention also relates to novel chlorinated derivatives of pantoprazole including 5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)-chloromethyl]sulfinyl]-1H-benzimidazole and 5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)-chlorohydroxymethyl]sulfinyl]-1H-benzimidazole and processes for making them. The invention also relates to processes of quantifying and identifying a compound other than pantoprazole in a mixture of pantoprazole and at least one other compound.

    摘要翻译： 本发明提供了一种方法，其包括将硫醚与约1.05至约1.6摩尔当量的活性氯氧化剂，优选次氯酸钠和约2.5至约5.0摩尔当量碱金属碱混合; 并回收优选泮托拉唑，兰索拉唑，奥美拉唑或雷贝拉唑的亚砜。 该方法可以进一步包括使亚砜与钠离子源（优选氢氧化钠）接触以产生亚砜的钠盐。 本发明还涉及泮托拉新的氯化衍生物，包括5-（二氟甲氧基）-2 - [[（3,4-二甲氧基-2-吡啶基） - 氯甲基]亚磺酰基] -1H-苯并咪唑和5-（二氟甲氧基）-2- [[（3,4-二甲氧基-2-吡啶基） - 氯羟甲基]亚磺酰基] -1H-苯并咪唑及其制备方法。 本发明还涉及在泮托拉唑和至少一种其它化合物的混合物中量化和鉴定泮托拉唑以外的化合物的方法。