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    PROCESSES FOR PREPARING EZETIMIBE AND INTERMEDIATE COMPOUNDS USEFUL FOR THE PREPARATION THEREOF
    1.
    发明申请
    PROCESSES FOR PREPARING EZETIMIBE AND INTERMEDIATE COMPOUNDS USEFUL FOR THE PREPARATION THEREOF 审中-公开
    制备EZETIMIBE和中间体化合物的方法可用于制备它们

    公开(公告)号：US20100168414A1

    公开(公告)日：2010-07-01

    申请号：US12295442

    申请日：2007-09-29

    申请人： Ana Gavalda Escude ,  Jordi Bosch i Llado ,  Ulrike Nettekoven

    发明人： Ana Gavalda Escude ,  Jordi Bosch i Llado ,  Ulrike Nettekoven

    IPC分类号： C07D205/08

    CPC分类号： C07D205/08 ,  Y02P20/55

    摘要： The invention relates, in general, to an improved process for converting compounds of Formula II (below) to compounds of Formula III (below), which are key intermediates for the synthesis of ezetimibe, or to ezetimibe itself, wherein in Formulas II and III, R represents hydrogen, alkyl, or a hydroxyl protecting group (e.g., benzyl group, a substituted benzyl group, or a silyl group). The invention further includes the use of the described process and the use of compounds of Formula III made by the described process for the preparation of ezetimibe.

    摘要翻译： 本发明一般涉及将式II化合物（下文）转化成式III化合物（下文）的改进方法，其是用于合成依泽替米贝或依泽替米贝本身的关键中间体，其中在式II和III中 ，R表示氢，烷基或羟基保护基（例如苄基，取代的苄基或甲硅烷基）。 本发明还包括所述方法的使用以及通过所述方法制备的式III化合物用于制备依泽替米贝的用途。

    Method For Determining Enantiomeric Purity Of Darifenacin And Intermediates
    3.
    发明申请
    Method For Determining Enantiomeric Purity Of Darifenacin And Intermediates 审中-公开
    达芬那敏和中间体对映体纯度的测定方法

    公开(公告)号：US20080312455A1

    公开(公告)日：2008-12-18

    申请号：US12138781

    申请日：2008-06-13

    申请人： Nuria Soldevilla Madrid ,  Jordi Bosch i Llado

    发明人： Nuria Soldevilla Madrid ,  Jordi Bosch i Llado

    IPC分类号： C07D405/06

    CPC分类号： G01N30/88 ,  B01D15/3833 ,  G01N30/02 ,  G01N2030/884 ,  G01N2030/8877

    摘要： The present invention relates to a method for differentiating and quantifying the enantiomers, thereby determining the enantiomeric purity, of darifenacin and its intermediate compounds and salts thereof. In addition, the invention relates to a method for differentiating and quantifying the enantiomers, thereby determining the enantiomeric purity of compounds of formula (I): wherein Y is hydrogen or a substituent of the formula: including the differentiation and quantification of compounds of formula (I) of varying enantiomeric purity from their corresponding enantiomers. The invention further relates to a process for preparing enantiomerically pure darifenacin using enantiomerically pure starting compounds which have been previously differentiated and quantified according to the method of the invention.

    摘要翻译： 本发明涉及用于分离和定量对映异构体的方法，从而确定达曲他辛及其中间体化合物及其盐的对映体纯度。 此外，本发明涉及用于分离和定量对映异构体的方法，从而确定式（I）化合物的对映体纯度：其中Y是氢或下式的取代基：包括式（I）化合物的分化和定量 I）与其相应的对映异构体不同的对映体纯度。 本发明还涉及使用已经根据本发明的方法预先分化和定量的对映体纯的起始化合物来制备对映体纯的达赖芬那肽的方法。