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    Process for production of lasofoxifene or analogue thereof
    5.
    发明授权
    Process for production of lasofoxifene or analogue thereof 有权
    雷诺昔芬或其类似物的生产方法

    公开(公告)号：US08193394B2

    公开(公告)日：2012-06-05

    申请号：US12162068

    申请日：2007-01-25

    申请人： Isamu Shiina ,  Yoshiyuki Sano ,  Kenya Nakata

    发明人： Isamu Shiina ,  Yoshiyuki Sano ,  Kenya Nakata

    IPC分类号： C07C33/02

    CPC分类号： C07C67/287 ,  C07C41/24 ,  C07C41/26 ,  C07C41/32 ,  C07C67/293 ,  C07C2602/10 ,  C07D295/084 ,  C07C69/63 ,  C07C69/24 ,  C07C43/23

    摘要： Disclosed is a novel process for production of lasofoxifene, nafoxidine or an analogue thereof, which comprises reduced number of reaction steps, has a high efficiency, and is practically advantageous. For the production of lasofoxifene or an analogue thereof, a compound represented by the formula (4) is used as an intermediate. The compound represented by the formula (4) can be produced using compounds represented by the formulae (1) to (3) as starting compounds by performing the coupling of the three components in one step.

    摘要翻译： 本发明公开了一种生产拉索昔芬，nafoxidine或其类似物的新方法，其包括减少数量的反应步骤，具有高效率，并且实际上是有利的。 为了生产拉索昔芬或其类似物，使用由式（4）表示的化合物作为中间体。 由式（4）表示的化合物可以通过在一个步骤中进行三种成分的偶联而使用由式（1）至（3）表示的化合物作为起始化合物来制备。

    Method for producing optically active 2-hydroxy ester and novel intermediate compound
    6.
    发明授权
    Method for producing optically active 2-hydroxy ester and novel intermediate compound 有权
    光学活性2-羟基酯和新型中间体化合物的制备方法

    公开(公告)号：US08552215B2

    公开(公告)日：2013-10-08

    申请号：US13255465

    申请日：2010-03-08

    申请人： Isamu Shiina ,  Kenya Nakata

    发明人： Isamu Shiina ,  Kenya Nakata

    IPC分类号： C07C69/013

    CPC分类号： C07B53/00 ,  C07B57/00 ,  C07B2200/07 ,  C07C67/08 ,  C07F7/1804 ,  C07C69/734

    摘要： Disclosed is a method for producing an optically active 2-hydroxy ester, comprising selectively esterifying one enantiomer of a racemic 2-hydroxy ester in a solvent containing a catalyst such as tetramisole or benzotetramisole, and a carboxylic acid anhydride, or a carboxylic acid anhydride and a carboxylic acid. In particular, in the case where the solvent contains a carboxylic acid anhydride, but does not contain a carboxylic acid, as the carboxylic acid anhydride, a carboxylic acid anhydride containing a tertiary or quaternary carbon atom in the a-position is used. On the other hand, in the case where the solvent contains a carboxylic acid anhydride and a carboxylic acid, as the carboxylic acid, a carboxylic acid containing a tertiary or quaternary carbon atom in the a-position is used.

    摘要翻译： 公开了一种光学活性2-羟基酯的制备方法，该方法包括选择性地酯化含有催化剂的溶剂中的外消旋2-羟基酯的一种对映异构体，所述催化剂如四聚甲基或苯并四唑，以及羧酸酐或羧酸酐， 羧酸。 特别是在溶剂含有羧酸酐但不含有羧酸的情况下，作为羧酸酐，使用在a位含有叔或季碳原子的羧酸酐。 另一方面，在溶剂含有羧酸酐和羧酸的情况下，作为羧酸，使用在a位具有叔或季碳原子的羧酸。

    METHOD FOR PRODUCING OPTICALLY ACTIVE 2-HYDROXY ESTER AND NOVEL INTERMEDIATE COMPOUND
    7.
    发明申请
    METHOD FOR PRODUCING OPTICALLY ACTIVE 2-HYDROXY ESTER AND NOVEL INTERMEDIATE COMPOUND 有权
    用于生产光学活性2-羟基酯和新型中间体化合物的方法

    公开(公告)号：US20110319650A1

    公开(公告)日：2011-12-29

    申请号：US13255465

    申请日：2010-03-08

    申请人： Isamu Shiina ,  Kenya Nakata

    发明人： Isamu Shiina ,  Kenya Nakata

    IPC分类号： C07C69/76 ,  C07C69/00

    CPC分类号： C07B53/00 ,  C07B57/00 ,  C07B2200/07 ,  C07C67/08 ,  C07F7/1804 ,  C07C69/734

    摘要： Disclosed is a method for producing an optically active 2-hydroxy ester, comprising selectively esterifying one enantiomer of a racemic 2-hydroxy ester in a solvent containing a catalyst such as tetramisole or benzotetramisole, and a carboxylic acid anhydride, or a carboxylic acid anhydride and a carboxylic acid. In particular, in the case where the solvent contains a carboxylic acid anhydride, but does not contain a carboxylic acid, as the carboxylic acid anhydride, a carboxylic acid anhydride containing a tertiary or quaternary carbon atom in the a-position is used. On the other hand, in the case where the solvent contains a carboxylic acid anhydride and a carboxylic acid, as the carboxylic acid, a carboxylic acid containing a tertiary or quaternary carbon atom in the a-position is used.

    摘要翻译： 公开了一种光学活性2-羟基酯的制备方法，该方法包括选择性地酯化含有催化剂的溶剂中的外消旋2-羟基酯的一种对映异构体，所述催化剂如四聚甲基或苯并四唑，以及羧酸酐或羧酸酐， 羧酸。 特别是在溶剂含有羧酸酐但不含有羧酸的情况下，作为羧酸酐，使用在a位含有叔或季碳原子的羧酸酐。 另一方面，在溶剂含有羧酸酐和羧酸的情况下，作为羧酸，使用在a位具有叔或季碳原子的羧酸。

    Process for Production of Lasofoxifene or Analogue Thereof
    8.
    发明申请
    Process for Production of Lasofoxifene or Analogue Thereof 有权
    拉索昔芬或其类似物的生产工艺

    公开(公告)号：US20090012314A1

    公开(公告)日：2009-01-08

    申请号：US12162068

    申请日：2007-01-25

    申请人： Isamu Shiina ,  Yoshiyuki Sano ,  Kenya Nakata

    发明人： Isamu Shiina ,  Yoshiyuki Sano ,  Kenya Nakata

    IPC分类号： C07D207/04 ,  C07C43/20 ,  C07C41/01

    CPC分类号： C07C67/287 ,  C07C41/24 ,  C07C41/26 ,  C07C41/32 ,  C07C67/293 ,  C07C2602/10 ,  C07D295/084 ,  C07C69/63 ,  C07C69/24 ,  C07C43/23

    摘要： Disclosed is a novel process for production of lasofoxifene, nafoxidine or an analogue thereof, which comprises reduced number of reaction steps, has a high efficiency, and is practically advantageous. For the production of lasofoxifene or an analogue thereof, a compound represented by the formula (4) is used as an intermediate. The compound represented by the formula (4) can be produced using compounds represented by the formulae (1) to (3) as starting compounds by performing the coupling of the three components in one step.

    摘要翻译： 本发明公开了一种生产拉索昔芬，nafoxidine或其类似物的新方法，其包括减少数量的反应步骤，具有高效率，并且实际上是有利的。 为了生产拉索昔芬或其类似物，使用由式（4）表示的化合物作为中间体。 由式（4）表示的化合物可以通过在一个步骤中进行三种成分的偶联而使用由式（1）至（3）表示的化合物作为起始化合物来制备。