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    Process for Preparing Benzhydrylthioacetamide
    6.
    发明申请
    Process for Preparing Benzhydrylthioacetamide 失效
    制备二苯甲基硫代乙酰胺的方法

    公开(公告)号：US20080027240A1

    公开(公告)日：2008-01-31

    申请号：US10570243

    申请日：2004-10-22

    申请人： Sidney Liang

    发明人： Sidney Liang

    IPC分类号： C07C323/51 ,  C07C317/44

    CPC分类号： C07C319/14 ,  C07C315/02 ,  C07C317/44 ,  C07C323/52

    摘要： The present invention is directed to an improved process for preparing modafinil wherein benzhydrylthioacetate is prepared in high yield and purity by the reaction of a haloacetate with the reaction product of thiourea and benzhydrol. The reaction employing the haloacetate is conducted in a solvent comprising an organic solvent such as methanol having dissolved therein an organic base or an inorganic basic salt such as sodium bicarbonate. The resulting benzhydrylthioacetate can be amidated and then oxidized to provide the pharmaceutical grade modafinil in high yield and purity.

    摘要翻译： 本发明涉及一种制备莫替非尼的改进方法，其中通过卤代乙酸酯与硫脲和二苯甲醛的反应产物的反应，以高产率和纯度制备二苯甲基硫代乙酸乙酯。 使用卤代乙酸酯的反应在包括有机溶剂如甲醇中溶解有有机碱或无机碱性盐如碳酸氢钠的溶剂中进行。 所得的二苯甲基硫代乙酸酯可以酰胺化，然后氧化，以高产率和纯度提供药物级莫达非因。

    Crystalline Forms of Levorphanol
    7.
    发明申请
    Crystalline Forms of Levorphanol 审中-公开
    左旋啡多晶的形式

    公开(公告)号：US20070281957A1

    公开(公告)日：2007-12-06

    申请号：US11753012

    申请日：2007-05-24

    申请人： Sidney Liang ,  Gary A. Nichols ,  Michelle R. Menze

    发明人： Sidney Liang ,  Gary A. Nichols ,  Michelle R. Menze

    IPC分类号： A61K31/485 ,  C07D489/02

    CPC分类号： C07D221/28

    摘要： The present invention relates to novel crystalline polymorphic forms of levorphanol including hydrated, solvated, and non-hydrated (non-solvated) forms. The invention also describes methods of preparing the various polymorphic forms. The present invention also relates to pharmaceutical compositions containing crystalline polymorphs of levorphanol, as well as methods of relieving pain by administering the pharmaceutical compositions.

    摘要翻译： 本发明涉及左旋啡喃的新型结晶多晶型，包括水合，溶剂化和非水合（非溶剂化）形式。 本发明还描述了制备各种多晶型物的方法。 本发明还涉及包含左啡诺的结晶多晶型物的药物组合物，以及通过施用药物组合物来缓解疼痛的方法。

    Processes for the Preparation of Modafinil and Analogs Thereof
    8.
    发明申请
    Processes for the Preparation of Modafinil and Analogs Thereof 审中-公开
    莫达非尼及其类似物的制备方法

    公开(公告)号：US20080319227A1

    公开(公告)日：2008-12-25

    申请号：US12096624

    申请日：2006-11-27

    申请人： Sidney Liang ,  John R. Duchek ,  Carl J. Schaefer

    发明人： Sidney Liang ,  John R. Duchek ,  Carl J. Schaefer

    IPC分类号： C07C315/02

    CPC分类号： C07C315/02 ,  C07C317/44

    摘要： The present invention generally relates to an improved process for preparing modafinil and analogs thereof. The process minimizes impurities and improves the overall yield by oxidizing a modafinil intermediate compound in a reaction mixture including an alcohol and an organic acid at a ratio of from about 1:1 to about 80:1 (by volume).

    摘要翻译： 本发明一般涉及一种制备莫替非尼及其类似物的改进方法。 该方法通过在包含醇和有机酸的反应混合物中以约1:1至约80:1（体积比）的比例氧化莫达非尼中间体化合物来最小化杂质并提高总产率。

    Process for preparing benzhydrylthioacetamide
    9.
    发明申请
    Process for preparing benzhydrylthioacetamide 有权
    制备二苯甲基硫代乙酰胺的方法

    公开(公告)号：US20060160903A1

    公开(公告)日：2006-07-20

    申请号：US10537965

    申请日：2004-02-23

    申请人： Sidney Liang

    发明人： Sidney Liang

    IPC分类号： A61K31/165 ,  C07C323/39

    CPC分类号： C07C335/32 ,  C07C315/02 ,  C07C315/06 ,  C07C319/14 ,  C07C323/60 ,  C07C317/44

    摘要： The present invention is directed to an improved process for preparing modafinil wherein benzhydrylthioacetamide is prepared in high yield and purity by the reaction of a haloacetamide with the reaction product of thiourea and benzhydrol in aqueous solution. The reaction employing the haloacetamide is conducted in a solvent comprising water and an organic solvent such as dimethylformamide having dissolved therein a basic salt such as potassium carbonate. The resulting benzhydrylthioacetamide can be oxidized to provide the pharmaceutical modafinil.

    摘要翻译： 本发明涉及一种制备莫替非尼的改进方法，其中通过卤代乙酰胺与硫脲和二苯甲醇在水溶液中的反应产物的反应，以高产率和纯度制备二苯甲基硫代乙酰胺。 使用卤代乙酰胺的反应在包含水和有机溶剂如二甲基甲酰胺的溶剂中进行，其中溶解有碱性盐如碳酸钾。 所得的二苯甲基硫代乙酰胺可以被氧化以提供药物莫达非尼。

    Process for preparing benzhydrylthioacetamide
    10.
    发明授权
    Process for preparing benzhydrylthioacetamide 失效
    制备二苯甲基硫代乙酰胺的方法

    公开(公告)号：US07345188B2

    公开(公告)日：2008-03-18

    申请号：US10570243

    申请日：2004-10-22

    申请人： Sidney Liang

    发明人： Sidney Liang

    IPC分类号： C07C323/00 ,  C07C315/00 ,  C07C317/00

    CPC分类号： C07C319/14 ,  C07C315/02 ,  C07C317/44 ,  C07C323/52

    摘要： The present invention is directed to an improved process for preparing modafinil wherein benzhydrylthioacetate is prepared in high yield and purity by the reaction of a haloacetate with the reaction product of thiourea and benzhydrol. The reaction employing the haloacetate is conducted in a solvent comprising an organic solvent such as methanol having dissolved therein an organic base or an inorganic basic salt such as sodium bicarbonate. The resulting benzhydrylthioacetate can be amidated and then oxidized to provide the pharmaceutical grade modafinil in high yield and purity.

    摘要翻译： 本发明涉及一种制备莫替非尼的改进方法，其中通过卤代乙酸酯与硫脲和二苯甲醛的反应产物的反应，以高产率和纯度制备二苯甲基硫代乙酸乙酯。 使用卤代乙酸酯的反应在包括有机溶剂如甲醇中溶解有有机碱或无机碱性盐如碳酸氢钠的溶剂中进行。 所得的二苯甲基硫代乙酸酯可以酰胺化，然后氧化，以高产率和纯度提供药物级莫达非因。