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114 条记录 (耗时 0.024 秒)

    Processes for preparing 6-hydroxy-3,4-dihydroquinolinone, cilostazol and N-(4-methoxyphenyl)-3-chloropropionamide
    84.
    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。

    Torsemide polymorphs
    87.
    发明授权
    Torsemide polymorphs 失效
    泰索米多晶型物

    公开(公告)号：US06465496B1

    公开(公告)日：2002-10-15

    申请号：US09638106

    申请日：2000-08-11

    申请人： Judith Aronhime ,  David Leonov ,  Marko Kordova ,  Anchel Schwartz ,  Ben-Zion Dolitzky

    发明人： Judith Aronhime ,  David Leonov ,  Marko Kordova ,  Anchel Schwartz ,  Ben-Zion Dolitzky

    IPC分类号： A61K3144

    CPC分类号： C07D213/74 ,  A61K31/64

    摘要： The present invention is directed to the novel forms of torsemide, designated Form V, amorphous torsemide, Dupont Form 2 solvent adduct, Dupont Form 2 ethanol adduct and Dupont Form 2 isopropanol adduct. Methods for their preparation are also disclosed. The present invention also relates to processes for making torsemide modification I. Pharmaceutical compositions containing the new forms of torsemide and methods of using them are also disclosed.

    摘要翻译： 本发明涉及形式为V，无定形托塞米特，杜邦2型溶剂加合物，杜邦2型乙醇加合物和杜邦2型异丙醇加合物的新型托马斯。 还公开了它们的制备方法。 本发明还涉及制备托塞米特改性的方法I.还公开了含有新形式的托塞米的药物组合物及其使用方法。

    Crystalline forms of quetiapine hemifumarate
    88.
    发明申请
    Crystalline forms of quetiapine hemifumarate 审中-公开
    喹硫平半富马酸盐的结晶形式

    公开(公告)号：US20100016579A1

    公开(公告)日：2010-01-21

    申请号：US12455947

    申请日：2009-06-08

    申请人： Revital Lifshitz-Liron ,  Eti Kovalevski-Ishai ,  Ben-Zion Dolitzky ,  Shlomit Wizel ,  Rami Lidor-Hadas

    发明人： Revital Lifshitz-Liron ,  Eti Kovalevski-Ishai ,  Ben-Zion Dolitzky ,  Shlomit Wizel ,  Rami Lidor-Hadas

    IPC分类号： C07D417/04

    CPC分类号： C07D281/16

    摘要： The present invention relates to novel crystalline forms of quetiapine hemifumarate, denominated quetiapine hemifumarate form II and quetiapine hemifumarate form III. These novel crystalline forms of quetiapine hemifumarate have been characterized by methods including x-ray powder diffraction (XRD), Fourier transform IR spectroscopy (FTIR), differential scanning calorimetry (DSC), and thermal gravimetric analysis (TGA). Methods for preparation of the novel crystalline quetiapine hemifumarate form II as its chloroform solvate and its dichloromethane solvate, form III as its chloroform solvate, and form I are provided.

    摘要翻译： 本发明涉及喹硫平半富马酸盐的新型结晶形式，称为喹喔啉半富马酸盐形式II和喹硫平半富马酸盐形式III。 已经通过X射线粉末衍射（XRD），傅立叶变换红外光谱（FTIR），差示扫描量热法（DSC）和热重分析（TGA）等方法对这些新型的喹硫平半富马酸盐结晶形态进行了表征。 提供了形成II型作为其氯仿溶剂合物的新型结晶喹硫平半富马酸盐及其二氯甲烷溶剂合物，形式III为其氯仿溶剂合物和形式I的方法。

    Processes for the preparation of a linezolid intermediate, linezolid hydroxide
    90.
    发明申请
    Processes for the preparation of a linezolid intermediate, linezolid hydroxide 审中-公开
    制备利奈唑胺中间体，利奈唑烷氢氧化物的方法

    公开(公告)号：US20090093631A1

    公开(公告)日：2009-04-09

    申请号：US12231769

    申请日：2008-09-05

    申请人： Ben-Zion Dolitzky ,  Nurit Perlman ,  Marina Kalujny

    发明人： Ben-Zion Dolitzky ,  Nurit Perlman ,  Marina Kalujny

    IPC分类号： C07D413/10

    CPC分类号： C07D263/24 ,  C07D263/26

    摘要： Provided are methods for the enantiomeric purification of Linezolid hydroxide, comprising providing a solution or a slurry of Linezolid hydroxide and a solvent selected from alcohols and ketones and crystallizing Linezolid hydroxide from the solution or slurry to obtain Linezolid hydroxide with a low content of S isomer.

    摘要翻译： 本发明提供了利奈唑烷氢氧化物的对映异构体纯化方法，包括从溶液或浆液中提供选自醇和酮的溶剂或溶剂和选自醇和酮的溶剂和结晶的利奈唑烷，以获得具有低含量的S异构体的生产线型利唑烷。