光学活性β−フェニルアラニンの製造法
    5.
    发明申请
    光学活性β−フェニルアラニンの製造法 审中-公开
    生产光学活性β-苯乙胺的方法

    公开(公告)号:WO2003068728A1

    公开(公告)日:2003-08-21

    申请号:PCT/JP2003/001364

    申请日:2003-02-10

    发明人: 野平 博之

    IPC分类号: C07C231/20

    摘要: A process for production of optically active N-acetyl -beta-phenylalanine through optical resolution of N-acetyl-beta- phenylalanine by preferential crystallization. According to this process, not only optically active N-acetyl-beta-phenyl- alanine but also optically active beta-phenylalanine can be produced easily and efficiently.

    摘要翻译: 通过优先结晶通过光学拆分N-乙酰基-β-苯丙氨酸生产光学活性N-乙酰基 - 苯丙氨酸的方法。 根据该方法,不仅可以容易且有效地制备光学活性的N-乙酰基-β-苯基 - 丙氨酸,而且还可以制备光学活性的β-苯丙氨酸。

    HYDROLYSIS OF ACYLAMINO ACIDS
    6.
    发明申请
    HYDROLYSIS OF ACYLAMINO ACIDS 审中-公开
    丙氨酸的水解

    公开(公告)号:WO02014260A1

    公开(公告)日:2002-02-21

    申请号:PCT/EP2001/008257

    申请日:2001-07-18

    摘要: The invention provides a process for the preparation of racemic amino acids, characterized in that an acylamino acid of the general formula R -CH(NH-CO-R )COOH wherein R is hydrogen, a linear, branched or cyclic alkyl radical that has from 1 to 7 carbon atoms and that may contain substituents such as a hydroxyl, alkyloxy or alkylthio group; and R is a hydrogen atom or an alkyl radical having from 1 to 3 carbon atoms; is heated in the presence of water, in a pressure-resistant vessel, to a temperature in the range from 110 DEG C to 220 DEG C and is hydrolyzed.

    摘要翻译: 本发明提供了制备外消旋氨基酸的方法,其特征在于通式为R 1 -CH(NH-CO-R 2)COOH的酰氨基酸,其中R 1为氢,线性 具有1至7个碳原子并且可以含有取代基如羟基,烷氧基或烷硫基的支链或环状烷基; 和R 2是氢原子或具有1至3个碳原子的烷基; 在水的存在下,在耐压容器中加热至110℃至220℃的温度并水解。

    MANUFACTURING PROCESS FOR SITAGLIPTIN FROM L-ASPARTIC ACID
    10.
    发明申请
    MANUFACTURING PROCESS FOR SITAGLIPTIN FROM L-ASPARTIC ACID 审中-公开
    来自L-天冬酰胺的西他汀的制备方法

    公开(公告)号:WO2012156888A1

    公开(公告)日:2012-11-22

    申请号:PCT/IB2012/052374

    申请日:2012-05-13

    发明人: SOUKUP, Milan

    摘要: The present invention relates to a novel manufacturing process of pharmaceutically active compound of formula (I) used as oral anti-diabetic drug. Starting from -aspartic acid derivate of formula (IV) the invention describes preparation of the chiral (R)-β-amino acid of formula (II) known as a precursor in the synthesis of Sitagliptin (Formula I). Formulae (I), (II) & (IV):

    摘要翻译: 本发明涉及用作口服抗糖尿病药物的式(I)药学活性化合物的新型制造方法。 从式(IV)的天冬氨酸衍生物开始,本发明描述了在西他列汀(式I)的合成中称为前体的式(II)的手性(R)-β-氨基酸的制备。 式(I),(II)和(IV):