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    PROCESS FOR PREPARING LERCANIDIPINE HYDROCHLORIDE
    1.
    发明申请
    PROCESS FOR PREPARING LERCANIDIPINE HYDROCHLORIDE 审中-公开
    制备氯卡吡啶盐酸盐的方法

    公开(公告)号：US20110040097A1

    公开(公告)日：2011-02-17

    申请号：US12521366

    申请日：2007-06-05

    申请人： Young-Deuck Kim ,  Jae-Yeon Shin

    发明人： Young-Deuck Kim ,  Jae-Yeon Shin

    IPC分类号： C07D211/90

    CPC分类号： C07D211/90

    摘要： Disclosed herein is a novel method for preparing lercanidipine hydrochloride which is highly effective for treating hypertension. The method comprises the steps of reacting 2,6-dimethyl-5-methoxycarbonyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3-carboxylic acid with a substituted chlorophosphate derivative to obtain a substituted phosphonoester derivative, and reacting the substituted phosphonoester derivative with 2, N-dimethyl-N-(3,3-diphenylpropyl)-1-amino-2-propanol. According to the preparation method, since little by-products are formed, the yield is improved, as compared to cases of conventional methods. In addition, the method involves simple isolation and purification processes of lercanidipine, thus realizing a high-quality product. Furthermore, the method has advantages of low preparation costs, substantial waste-free environmental-friendly process and applicability to industrial mass-production.

    摘要翻译： 本文公开了一种制备氯卡地平盐酸盐的新方法，其对于治疗高血压是非常有效的。 该方法包括以下步骤：使2,6-二甲基-5-甲氧基羰基-4-（3-硝基苯基）-1,4-二氢吡啶-3-羧酸与取代的氯磷酸酯衍生物反应，得到取代的膦酰酯衍生物， 取代的膦酰酯衍生物与2，N-二甲基-N-（3,3-二苯基丙基）-1-氨基-2-丙醇。 根据制备方法，与常规方法相比，由于形成少量副产物，产率提高。 此外，该方法涉及氯卡地平的简单隔离和纯化过程，从而实现了高品质的产品。 此外，该方法具有制备成本低，实质性无废物环保工艺和工业批量生产的适用性的优点。

    Process for preparing 2′-deoxy-2′, 2′-difluorocytidine
    2.
    发明授权
    Process for preparing 2′-deoxy-2′, 2′-difluorocytidine 失效
    制备2'-脱氧-2'，2'-二氟胞苷的方法

    公开(公告)号：US07994310B2

    公开(公告)日：2011-08-09

    申请号：US12532331

    申请日：2008-03-20

    申请人： Su-Jin Park ,  Chun-Rim Oh ,  Young-Deuck Kim

    发明人： Su-Jin Park ,  Chun-Rim Oh ,  Young-Deuck Kim

    IPC分类号： C07H19/073

    CPC分类号： C07H1/00 ,  C07H19/06 ,  Y02P20/55

    摘要： Disclosed is a method for preparing 2′-deoxy-2′,2′-difluorocytidine of Formula I comprising, preparing an optically pure 3R-hydroxypropane amide compound of Formula VIII from an optical ester compound of Formula IX using an optically active chiral amine, preparing an optically pure D-erythro-2,2-difluoro-2-deoxy-1-oxoribose compound of Formula V from the compound of Formula VIII, glycosylating the compound of Formula V with a nucleobase to prepare the 2′-deoxy-2′,2′-difluorocytidine of Formula I as a β-nucleoside. With the present invention, it is possible to prepare an optically pure compound of Formula I in a high purity and a high yield. In the Formulae, R1 and R2 are protecting groups and are each independently benzoyl, 4-methylbenzoyl, 3-methylbenzoyl, 4-cyanobenzoyl, 3-cyanobenzoyl, 4-propylbenzoyl, 2-ethoxybenzoyl, 4-t-butylbenzoyl, 1-naphthoyl or 2-naphthoyl, R3, R4 and R7 are each independently C1-C3 alkyl, R5 is methyl or ethyl, R6 is hydrogen, methyl or methoxy.

    摘要翻译： 公开了一种制备式I的2'-脱氧-2'，2'-二氟胞苷的方法，其包括：使用光学活性手性胺由式IX的光学酯化合物制备光学纯的3R-羟基丙酰胺化合物， 从式VIII化合物制备光学纯的D-型赤式-2,2-二氟-2-脱氧-1-氧代核糖核糖化合物，用式I化合物将式V化合物糖基化，从而制备2'-脱氧-2 '，式I的2'-二氟胞苷作为核苷。 通过本发明，可以以高纯度和高收率制备光学纯的式I化合物。 在式中，R 1和R 2是保护基，各自独立地是苯甲酰基，4-甲基苯甲酰基，3-甲基苯甲酰基，4-氰基苯甲酰基，3-氰基苯甲酰基，4-丙基苯甲酰基，2-乙氧基苯甲酰基，4-叔丁基苯甲酰基，1-萘甲酰基或 2-萘甲酰基，R3，R4和R7各自独立地为C1-C3烷基，R5为甲基或乙基，R6为氢，甲基或甲氧基。

    PROCESS FOR PREPARING OF 2'-DEOXY-2'2'-DIFLUOROCYTIDINE
    5.
    发明申请
    PROCESS FOR PREPARING OF 2'-DEOXY-2'2'-DIFLUOROCYTIDINE 失效
    制备2'-脱氧-2'-脱氧胆碱的方法

    公开(公告)号：US20100069625A1

    公开(公告)日：2010-03-18

    申请号：US12532331

    申请日：2008-03-20

    申请人： Su-Jin Park ,  Chun-Rim Oh ,  Young-Deuck Kim

    发明人： Su-Jin Park ,  Chun-Rim Oh ,  Young-Deuck Kim

    IPC分类号： C07H19/06 ,  C07H3/02 ,  C07D317/08

    CPC分类号： C07H1/00 ,  C07H19/06 ,  Y02P20/55

    摘要： Disclosed is a method for preparing 2′-deoxy-2′,2′-difluorocytidine of Formula I comprising, preparing an optically pure 3R-hydroxypropane amide compound of Formula VIII from an optical ester compound of Formula IX using an optically active chiral amine, preparing an optically pure D-erythro-2,2-difluoro-2-deoxy-1-oxoribose compound of Formula V from the compound of Formula VIII, glycosylating the compound of Formula V with a nucleobase to prepare the 2′-deoxy-2′,2′-difluorocytidine of Formula I as a β-nucleoside. With the present invention, it is possible to prepare an optically pure compound of Formula I in a high purity and a high yield. In the Formulae, R1 and R2 are protecting groups and are each independently benzoyl, 4-methylbenzoyl, 3-methylbenzoyl, 4-cyanobenzoyl, 3-cyanobenzoyl, 4-propylbenzoyl, 2-ethoxybenzoyl, 4-t-butylbenzoyl, 1-naphthoyl or 2-naphthoyl, R3, R4 and R7 are each independently C1-C3 alkyl, R5 is methyl or ethyl, R6 is hydrogen, methyl or methoxy.

    摘要翻译： 公开了一种制备式I的2'-脱氧-2'，2'-二氟胞苷的方法，其包括：使用光学活性手性胺由式IX的光学酯化合物制备光学纯的3R-羟基丙酰胺化合物， 从式VIII化合物制备光学纯的D-型赤式-2,2-二氟-2-脱氧-1-氧代核糖核糖化合物，用式I化合物将式V化合物糖基化，从而制备2'-脱氧-2 '，式Ⅰ的2'-二氟胞苷作为核苷。 通过本发明，可以以高纯度和高收率制备光学纯的式I化合物。 在式中，R 1和R 2是保护基，各自独立地是苯甲酰基，4-甲基苯甲酰基，3-甲基苯甲酰基，4-氰基苯甲酰基，3-氰基苯甲酰基，4-丙基苯甲酰基，2-乙氧基苯甲酰基，4-叔丁基苯甲酰基，1-萘甲酰基或 2-萘甲酰基，R3，R4和R7各自独立地为C1-C3烷基，R5为甲基或乙基，R6为氢，甲基或甲氧基。