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    Process for the production of optically active compounds having substituents at the 2-position
    1.
    发明申请
    Process for the production of optically active compounds having substituents at the 2-position 审中-公开
    用于制备在2-位具有取代基的光学活性化合物的方法

    公开(公告)号：US20060247458A1

    公开(公告)日：2006-11-02

    申请号：US10546823

    申请日：2004-02-25

    申请人： Shogo Yamamoto ,  Toshihiro Takeda ,  Yoshihide Fuse ,  Yasuyoshi Ueda

    发明人： Shogo Yamamoto ,  Toshihiro Takeda ,  Yoshihide Fuse ,  Yasuyoshi Ueda

    IPC分类号： C07C319/02

    CPC分类号： C07B53/00 ,  C07B2200/07 ,  C07C51/363 ,  C07C319/14 ,  C07C57/58 ,  C07C323/56

    摘要： The present invention provides a process for producing an optically active compound having a thio group at the 2-position important for manufacturing medicines. An optically active compound having a hydroxyl group at the 2-position is chlorinated with inversion of the configuration at the 2-position, and the resultant optically active compound having a chlorine atom at the 2-position is reacted with a metal thiolate to introduce a thio group with inversion of the configuration at the 2-position. This process is capable of minimizing racemization and producing an optically active compound having a thio group at the 2-position at low cost in high yield. When the optically active compound having a chlorine atom at the 2-position is reacted with the metal thiolate in coexistence with water in the reaction system, the optically active compound having a thio group at the 2-position with higher optical purity can be produced in higher yield. An optically active carboxylic acid having a thio group at the 2-position is crystallized in the presence of an aliphatic hydrocarbon solvent and/or a sulfur-containing solvent to effectively remove coexistent impurities such as an optical isomer and the like, thereby producing crystals of an optically active carboxylic acid having a thio group at the 2-position with higher purity.

    摘要翻译： 本发明提供了制造药物重要的2位具有硫基的光学活性化合物的方法。 在2-位上具有羟基的光学活性化合物用2-位反转形式进行氯化，所得2-位上具有氯原子的光学活性化合物与金属硫醇盐反应，引入 硫基与2-位配位反转。 该方法能够使外消旋化最小化，并以高产率以低成本制备在2-位具有硫基的光学活性化合物。 当反应体系中2-位上具有氯原子的光学活性化合物与金属硫醇盐在水中共存时，具有较高光学纯度的2位具有硫基的光学活性化合物可以在 更高的产量。 在脂肪族烃溶剂和/或含硫溶剂的存在下，在2-位具有硫基的光学活性羧酸结晶化，以有效除去共同的杂质如旋光异构体等，从而产生 在2-位具有较高纯度的具有硫基的光学活性羧酸。

    Process for producing 3-amino-2-hydroxypropionic acid derivatives
    8.
    发明授权
    Process for producing 3-amino-2-hydroxypropionic acid derivatives 失效
    3-氨基-2-羟基丙酸衍生物的制备方法

    公开(公告)号：US07057066B2

    公开(公告)日：2006-06-06

    申请号：US10312208

    申请日：2001-06-26

    申请人： Hiroshi Murao ,  Koki Yamashita ,  Toshihiro Takeda ,  Yasuyoshi Ueda

    发明人： Hiroshi Murao ,  Koki Yamashita ,  Toshihiro Takeda ,  Yasuyoshi Ueda

    IPC分类号： C07C229/06 ,  C07C229/34

    CPC分类号： C07D263/20 ,  C07C227/20 ,  C07C227/32 ,  C07C227/42 ,  Y02P20/55 ,  C07C229/22 ,  C07C229/34

    摘要： The present invention provides a process for preparing 3-amino-2-hydroxypropionic acid derivatives (1) which does not use dangerous reagents, is economically advantageous, and is suitable for an industrial production, which process comprises: treating N-protected-3-amino-2-hydroxypropionic acid derivatives (2) having a steric configuration at 2-position carbon reverse to that of derivatives (1) with a leaving group-introducing agent to convert into N-protected-3-aminopropionic acid derivatives (3), then treating the derivatives with a basic substance to convert into substituted-3-amino-2-hydroxypropionic acid derivatives (4) having an inverted steric configuration at 2-position carbon, and then converting the derivatives into 3-amino-2-hydroxypropionic acid derivatives (1).

    摘要翻译： 本发明提供了一种制备不使用危险试剂的3-氨基-2-羟基丙酸衍生物（1）的方法，在经济上是有利的，适用于工业生产，该方法包括：将N-保护的3- 具有与衍生物（1）相反的2-位碳位置的氨基-2-羟基丙酸衍生物（2）与离去基团引入剂转化为N-保护的3-氨基丙酸衍生物（3）， 然后用碱性物质处理衍生物，将其转化成在2-位碳上具有反向立体构型的取代-3-氨基-2-羟基丙酸衍生物（4），然后将其转化为3-氨基-2-羟基丙酸 衍生物（1）。

    Processes for preparing oxazolidinone derivatives of β-hydroxyethlamine compounds and for preparing β-hydroxyethlamine compounds
    10.
    发明授权
    Processes for preparing oxazolidinone derivatives of β-hydroxyethlamine compounds and for preparing β-hydroxyethlamine compounds 失效
    制备β-羟基三甲基胺化合物的恶唑烷酮衍生物和制备β-羟基三甲基胺化合物的方法

    公开(公告)号：US07307184B2

    公开(公告)日：2007-12-11

    申请号：US10478439

    申请日：2002-05-23

    申请人： Hiroshi Murao ,  Koki Yamashita ,  Toshihiro Takeda ,  Yasuyoshi Ueda

    发明人： Hiroshi Murao ,  Koki Yamashita ,  Toshihiro Takeda ,  Yasuyoshi Ueda

    IPC分类号： C07C269/00 ,  C07C269/06

    CPC分类号： C07D263/24 ,  C07D263/22

    摘要： The present invention provides a process of starting from N-alkoxycarbonyl-ethylamine compounds having a leaving group at the β-position to prepare oxazolidinone derivatives of β-hydroxyethylamine compounds having an inverted steric configuration at the β-position carbon, which comprises introducing a step of treating in contact with water with heating under acidic to neutral conditions into the process. Also, the present invention provides a process of starting from N-alkoxycarbonyl-ethylamine compounds having a leaving group at the β-position to prepare β-hydroxyethylamine compounds having an inverted steric configuration at the β-position carbon, which comprises subjecting the oxazolidinone derivatives prepared as described above to a step of treating in contact with water under basic conditions.

    摘要翻译： 本发明提供了从在β-位上具有离去基团的N-烷氧基羰基 - 乙胺化合物开始以制备β-位羟基化合物的恶唑烷酮衍生物的方法，所述β-羟乙基胺化合物在β-位置碳具有反向立体构型，其包括引入步骤 在酸性到中性条件下加热处理与水接触。 此外，本发明提供了从在β-位上具有离去基团的N-烷氧基羰基 - 乙胺化合物开始以制备在β-位置碳具有反向立体构型的β-羟乙基胺化合物的方法，该方法包括使恶唑烷酮衍生物 如上所述制备成在碱性条件下与水接触的步骤。