Sertraline hydrochloride polymorphs
    33.
    发明授权
    Sertraline hydrochloride polymorphs 有权
    舍曲林盐酸多晶型物

    公开(公告)号:US07022881B2

    公开(公告)日:2006-04-04

    申请号:US10861274

    申请日:2004-06-04

    IPC分类号: C07C211/00

    摘要: The present invention is directed to forms II, III, V, VI, VII, VIII, IX and X of sertraline hydrochloride and novel methods for their preparation. According to the present invention, sertraline hydrochloride polymorph II may be produced by slurrying sertraline hydrochloride polymorph VI in aprotic organic solvent. Sertraline hydrochloride polymorphic form III may be produced by heating sertraline hydrochloride polymorphs V and VI. Sertraline hydrochloride forms V and VI may be produced from either sertraline hydrochloride or sertraline base by crystallization. Sertraline hydrochloride Form VII may be produced by suspending sertraline chloride polymorph V in water, followed by filtration. Sertraline hydrochloride Forms VIII and IX may be produced by suspending sertraline base in water followed by acidification and filtration. Sertraline hydrochloride Form X may be produced by suspending sertraline hydrochloride in benzyl alcohol with heating, followed by filtration.

    摘要翻译: 本发明涉及舍曲林盐酸盐的形式II,III,V,VI,VII,VIII,IX和X及其制备方法。 根据本发明,盐酸舍曲林多晶型II可以通过将盐酸舍曲林多晶型VI制成非质子有机溶剂来制备。 舍曲林盐酸盐多晶型III可以通过加热舍曲林盐酸盐多晶型物V和VI来制备。 舍曲林盐酸盐形成V和VI可以通过结晶从舍曲林盐酸盐或舍曲林碱产生。 盐酸舍曲林形式VII可以通过将盐酸舍曲林多晶型V悬浮在水中,然后过滤来制备。 盐酸舍曲林形式VIII和IX可以通过将舍曲林碱悬浮在水中然后酸化和过滤来制备。 舍曲林盐酸盐形式X可以通过在加热下将舍曲林盐酸舍曲林悬浮在苄醇中,然后过滤来制备。

    Process for the preparation of 1,2-benzisoxazole-3-acetic acid
    38.
    发明授权
    Process for the preparation of 1,2-benzisoxazole-3-acetic acid 失效
    1,2-苯并异恶唑-3-乙酸的制备方法

    公开(公告)号:US06677458B2

    公开(公告)日:2004-01-13

    申请号:US10090710

    申请日:2002-03-04

    IPC分类号: C07D26120

    CPC分类号: C07D261/20

    摘要: The present invention provides a process for preparing 1,2-benzisoxazole-3-acetic acid, comprising the step of reacting 4-hydroxy-coumarin with hydroxyl-amine in the presence of a base. The present invention further provides a process for preparing a salt of benzisoxazole methane sulfonic acid, comprising the steps of 1) sulfonating 1,2-benzisoxazole-3-acetic acid using chlorosulfonic acid in a solvent mixture comprising methylene chloride and sodium hydroxide; and 2) isolating the salt of benzisoxazole methane sulfonic acid.

    摘要翻译: 本发明提供了制备1,2-苯并异恶唑-3-乙酸的方法,包括在碱存在下使4-羟基香豆素与羟胺反应的步骤。 本发明还提供了一种制备苯并异恶唑甲磺酸盐的方法,包括以下步骤:1)使用氯磺酸在包含二氯甲烷和氢氧化钠的溶剂混合物中磺化1,2-苯并异恶唑-3-乙酸; 和2)分离苯并异恶唑甲磺酸的盐。

    Sertraline hydrochloride polymorphs
    39.
    发明授权
    Sertraline hydrochloride polymorphs 有权
    舍曲林盐酸多晶型物

    公开(公告)号:US06500987B1

    公开(公告)日:2002-12-31

    申请号:US09448985

    申请日:1999-11-24

    IPC分类号: C07C21100

    摘要: The present invention is directed to forms II, III, V, VI, VII, VIII, IX and X of sertraline hydrochloride and novel methods for their preparation. According to the present invention, sertraline hydrochloride polymorph II may be produced by slurrying sertraline hydrochloride polymorph VI in aprotic organic solvent. Sertraline hydrochloride polymorphic form III may be produced by heating sertraline hydrochloride polymorphs V and VI. Sertraline hydrochloride forms V and VI may be produced from either sertraline hydrochloride or sertraline base by crystallization. Sertraline hydrochloride Form VII may be produced by suspending sertraline chloride polymorph V in water, followed by filtration. Sertraline hydrochloride Forms VIII and IX may be produced by suspending sertraline base in water followed by acidification and filtration. Sertraline hydrochloride Form X may be produced by suspending sertraline hydrochloride in benzyl alcohol with heating, followed by filtration.

    摘要翻译: 本发明涉及舍曲林盐酸盐的形式II,III,V,VI,VII,VIII,IX和X及其制备方法。 根据本发明,盐酸舍曲林多晶型II可以通过将盐酸舍曲林多晶型VI制成非质子有机溶剂来制备。 舍曲林盐酸盐多晶型III可以通过加热舍曲林盐酸盐多晶型物V和VI来制备。 舍曲林盐酸盐形成V和VI可以通过结晶从舍曲林盐酸盐或舍曲林碱产生。 盐酸舍曲林形式VII可以通过将舍曲林氯化物多晶型V悬浮在水中,然后过滤来制备。 盐酸舍曲林形式VIII和IX可以通过将舍曲林碱悬浮在水中然后酸化和过滤来制备。 舍曲林盐酸盐形式X可以通过在加热下将舍曲林盐酸舍曲林悬浮在苄醇中,然后过滤来制备。