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    • 2. 发明申请
    • METHOD FOR PRODUCING a-SUBSTITUTED CYSTEINE OR SALT THEREOF OR SYNTHETIC INTERMEDIATE OF a-SUBSTITUTED CYSTEINE
    • 生产取代的CYSTEINE或其盐的方法或其取代的CYSTEINE的合成中间体
    • US20160083341A1
    • 2016-03-24
    • US14888576
    • 2014-05-01
    • API Corporation
    • Yuuki AsumaHisatoshi UeharaTomoko MaedaYasuyo SaitoRyoma MiyakeHiroshi Kawabata
    • C07C319/06C07C323/52C12P13/12C07C323/58C07D277/14C07C319/14C07C319/20C07C323/60
    • C07C319/06C07C319/02C07C319/14C07C319/20C07C323/52C07C323/58C07C323/60C07D277/14C12P13/12C07C323/12C07C323/03
    • According to the present invention, it becomes possible to perform a process for converting into an α-substituted cysteine represented by general formula (1) or a salt thereof at low cost and on an industrial scale by employing a process that is routed through a compound represented by general formula (3) to a compound represented by general formula (6). Particularly, by employing a process that is routed through a compound represented by general formula (7-2), it becomes possible to detach a tert-butyl protection group in a simple manner and to produce the compound represented by general formula (1) with high purity. Furthermore, by employing a process that is routed through tert-butylthiomethanol or a process that is routed through a compound represented by general formula (9), it becomes possible to produce a compound represented by general formula (2) without generating bischloromethylether that is an oncogenic substance. In the production of an α-substituted-D-cysteine or a salt thereof, it becomes possible to perform a process for converting the compound represented by general formula (2) into a compound represented by general formula (3S) in one step by allowing an enzyme or the like to act on the compound represented by general formula (2).
    • 根据本发明,可以通过使用通过化合物的方法,以低成本和工业规模进行转化成由通式(1)表示的α-取代的半胱氨酸或其盐的方法 由通式(3)表示的化合物与通式(6)表示的化合物反应。 特别是通过使用通过通式(7-2)表示的化合物的方法,可以简单地分离叔丁基保护基,并制备通式(1)表示的化合物与 高纯度 此外,通过使用通过叔丁基硫醇的方法或通过通式(9)表示的化合物的方法,可以生成由通式(2)表示的化合物,而不产生作为 致癌物质。 在制备α-取代-D-半胱氨酸或其盐时,可以通过以下步骤进行将由通式(2)表示的化合物转化为通式(3S)表示的化合物的方法:允许 酶等作用于由通式(2)表示的化合物。