A process for the resolution of racemic verapamil
    57.
    发明公开
    A process for the resolution of racemic verapamil 审中-公开
    Verfahren zurLösungvon racemischen维拉帕米

    公开(公告)号:EP2014644A1

    公开(公告)日:2009-01-14

    申请号:EP08157735.5

    申请日:2008-06-06

    申请人: Cosma S.p.A.

    IPC分类号: C07C253/32 C07C255/43

    摘要: A new process is described for the resolution of racemic verapamil, which allows the desired enantiomer to be obtained in high yields and with high enantiomeric purity. The process uses optically active 2,3-bis[(2-fluorobenzoyl)oxy]butanedioic acid as the resolving agent, and a water/dimethylformamide or water/acetonitrile or water/methanol mixture, as the reaction solvent.

    摘要翻译: 描述了用于拆分外消旋维拉帕米的新方法,其允许以高产率和高对映体纯度获得所需的对映异构体。 该方法使用光学活性2,3-双[(2-氟苯甲酰基)氧基]丁二酸作为拆分剂,和水/二甲基甲酰胺或水/乙腈或水/甲醇混合物作为反应溶剂。

    Process for producing erythro-3-amino-2-hydroxybutyric acid derivatives
    58.
    发明公开
    Process for producing erythro-3-amino-2-hydroxybutyric acid derivatives 审中-公开
    Verfahren zur Herstellung von Erythro 3-Amino-2-Hydroxybuttersäurederivaten

    公开(公告)号:EP1464638A1

    公开(公告)日:2004-10-06

    申请号:EP04290652.9

    申请日:2000-06-22

    申请人: DAISO CO., LTD.

    摘要: A process for producing an erythro-3-amino-2-hydroxybutyric acid derivative characterized in that an erythro-3-amino-2-hydroxybutyronitrile derivative represented by the general formula [II]
    (wherein R 1 is a straight-chain, branched or cyclic alkyl group having one to six carbon atoms, an alkylthio group or an arylthio group having one to eight carbon atoms, or a substituted or unsubstituted aryl group, P 1 and P 2 are, the same or different, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aralkyloxycarbonyl group, a substituted or unsubstituted arylcarbonyl group, or a substituted or unsubstituted arylsulfonyl group, and R 2 is an alkylcarbonyl group, or a substituted or unsubstituted arylcarbonyl group), is treated with an acid in water or in a water-containing solvent to convert it into an erythro-3-amino-2-hydroxybutyric acid derivative represented by the general formula [III]
    (wherein R 1 is the same as mentioned above, R 3 is hydrogen, Q 1 and Q 2 are, the same or different, hydrogen, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted arylsulfonyl group), or the nitrile derivative is treated with an acid in an alcoholic solvent represented by the general formula of R 3 OH to convert it into an ester of the butyric acid represented by the above general formula [III] (R 3 is a straight-chain, branched or cyclic alkyl group having one to six carbon atoms, or a substituted or unsubstituted aralkyl group).

    摘要翻译: 一种制备赤式3-氨基-2-羟基丁酸衍生物的方法,其特征在于由通式ÄIIÜ表示的赤式-3-氨基-2-羟基丁腈衍生物(其中R 1是直链,支链或 具有1至6个碳原子的环烷基,具有1-8个碳原子的烷硫基或芳硫基,或取代或未取代的芳基,P1和P2相同或不同,取代或未取代的芳烷基, 取代或未取代的芳烷氧基羰基,取代或未取代的芳基羰基或取代或未取代的芳基磺酰基,R 2为烷基羰基或取代或未取代的芳基羰基)用酸在水中或含水 溶剂将其转化成由通式ÄIIIÜ表示的赤式3-氨基-2-羟基丁酸衍生物(其中R 1与上述相同,R 3是氢,Q 1 和Q2是相同或不同的氢,取代或未取代的芳烷基或取代或未取代的芳基磺酰基),或者腈衍生物用酸在通式R3OH表示的醇溶剂中进行处理以将其转化 由上述通式(III)表示的丁酸的酯(R3是具有1-6个碳原子的直链,支链或环状烷基或取代或未取代的芳烷基)。