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    • 5. 发明申请
    • Crystalline citalopram diol intermediate alkali
    • 结晶西酞普兰二醇中间体碱
    • US20070117992A1
    • 2007-05-24
    • US10583360
    • 2004-12-06
    • Runan MeiDianwu GuoShulong Wang
    • Runan MeiDianwu GuoShulong Wang
    • C07D307/81
    • C07D307/87C07C255/53
    • The present invention relates to the diol intermediate of citalopram useful for treatment of depression, that is to say, the crystal of free alkali of 3-hydroxylmethyl-4-[1-(4-fluorophenyl)-1-hydroxyl-4-(dimethylamino)] butylbenzonitrile and the method of crystallization thereof. The present invention has disclosed the method to prepare pure citalopram and its purified salts through crystallization of the described alkali;the optical resolution method of citalopram diol intermediate, the method to prepare S-citalopram and its purified salts by crystals mentioned above. The present invention has also disclosed the method to prepare citalopram and its purified salts, S-citalopram and its purified salts, as well as pharmaceutical formulation thereof obtained. Using methods of the present invention, the quality and yield of the product can be signally improved, and the production cost of the medicinal material can be decreased.
    • 本发明涉及可用于治疗抑郁症的西酞普兰的二醇中间体,也就是3-羟甲基-4- [1-(4-氟苯基)-1-羟基-4-(二甲基氨基 )]丁基苄腈及其结晶方法。 本发明公开了通过所述碱的结晶制备纯西酞普兰及其纯化盐的方法,西酞普兰二醇中间体的光学拆分方法,上述晶体制备S-西酞普兰及其纯化盐的方法。 本发明还公开了制备西酞普兰及其纯化盐S-西酞普兰及其纯化盐的方法及其药物制剂。 采用本发明的方法,可以显着提高产品的质量和产量,降低药材的生产成本。
    • 7. 发明授权
    • Crystalline citalopram diol intermediate alkali
    • 结晶西酞普兰二醇中间体碱
    • US07435838B2
    • 2008-10-14
    • US10583360
    • 2004-12-06
    • Runan MeiDianwu GuoShulong Wang
    • Runan MeiDianwu GuoShulong Wang
    • C07D307/78C07D307/87C07D307/93
    • C07D307/87C07C255/53
    • The present invention relates to the diol intermediate of citalopram useful for treatment of depression, which is the crystal of free base of 3-hydroxylmethyl-4-[1-(4-fluorophenyl)-1-hydroxyl-4-(dimethylamino)]butylbenzonitrile and the method of crystallization thereof. The present invention has disclosed the method to prepare pure citalopram and its purified salts through crystallization of the described base; the optical resolution method of citalopram diol intermediate, the method to prepare S-citalopram and its purified salts by crystals mentioned above. The present invention has also disclosed the method to prepare citalopram and its purified salts, S-citalopram and its purified salts, as well as pharmaceutical formulation thereof obtained. Using methods of the present invention, the quality and yield of the product can be significantly improved, and the production cost of the medicinal material can be reduced.
    • 本发明涉及可用于治疗抑郁症的西酞普兰的二醇中间体,其是3-羟甲基-4- [1-(4-氟苯基)-1-羟基-4-(二甲基氨基)]丁基苄腈的游离碱的晶体 及其结晶方法。 本发明公开了通过所述碱的结晶制备纯西酞普兰及其纯化盐的方法; 西酞普兰二元醇中间体的光学拆分方法,上述晶体制备S-西酞普兰及其纯化盐的方法。 本发明还公开了制备西酞普兰及其纯化盐S-西酞普兰及其纯化盐的方法及其药物制剂。 采用本发明的方法可以显着提高产品的质量和产量,降低药材的生产成本。