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    Process for the preparation of lacosamide
    1.
    发明授权
    Process for the preparation of lacosamide 有权
    制备漆酶的方法

    公开(公告)号：US08796488B2

    公开(公告)日：2014-08-05

    申请号：US13575152

    申请日：2010-12-22

    申请人： Alberto Bologna ,  Patrizia Castoldi ,  Domenico Vergani ,  Giorgio Bertolini

    发明人： Alberto Bologna ,  Patrizia Castoldi ,  Domenico Vergani ,  Giorgio Bertolini

    IPC分类号： C07C233/06 ,  C07C231/14 ,  C07C231/20 ,  C07C231/12 ,  C07C237/22 ,  C07C237/06

    CPC分类号： C07C237/22 ,  C07B2200/07 ,  C07C231/12 ,  C07C231/20 ,  C07C237/06

    摘要： A novel process for the synthesis of Lacosamide using D,L-serine as starting material is described, where the methylation reaction of hydroxyl is carried out using an inexpensive base such as NaOH and an inexpensive alkylating agent, non-toxic and non-carcinogenic, such as methyl p-toluenesulfonate; the R enantiomer is isolated from the racemic mixture of Lacosamide after selective hydrolysis of the acetamide, salification of the racemic mixture with a chiral acid (HX*) in an organic solvent, resolution of the diastereoisomeric mixture, preferably by precipitation of the R enantiomer, and subsequent acetylation of the optically pure intermediate.

    摘要翻译： 描述了使用D，L-丝氨酸作为起始原料合成Lacosamide的新方法，其中羟基的甲基化反应使用廉价的碱如NaOH和廉价的烷基化剂进行，无毒和非致癌， 如对甲苯磺酸甲酯; 选择性水解乙酰胺后，将R对映异构体与赖氨酰胺的外消旋混合物分离，用有机溶剂中的手性酸（HX *）进行外消旋混合物的成盐，非对映异构体混合物的拆分，优选通过沉淀R对映异构体， 和随后的光学纯中间体的乙酰化。

    PROCESS FOR THE PREPARATION OF LACOSAMIDE
    5.
    发明申请
    PROCESS FOR THE PREPARATION OF LACOSAMIDE 有权
    制备柠檬酰胺的方法

    公开(公告)号：US20130030216A1

    公开(公告)日：2013-01-31

    申请号：US13575152

    申请日：2010-12-22

    申请人： Alberto Bologna ,  Patrizia Castoldi ,  Domenico Vergani ,  Giorgio Bertolini

    发明人： Alberto Bologna ,  Patrizia Castoldi ,  Domenico Vergani ,  Giorgio Bertolini

    IPC分类号： C07C231/14 ,  C07C237/06

    CPC分类号： C07C237/22 ,  C07B2200/07 ,  C07C231/12 ,  C07C231/20 ,  C07C237/06

    摘要： A novel process for the synthesis of Lacosamide using D,L-serine as starting material is described, where the methylation reaction of hydroxyl is carried out using an inexpensive base such as NaOH and an inexpensive alkylating agent, non-toxic and non-carcinogenic, such as methyl p-toluenesulfonate; the R enantiomer is isolated from the racemic mixture of Lacosamide after selective hydrolysis of the acetamide, salification of the racemic mixture with a chiral acid (HX*) in an organic solvent, resolution of the diastereoisomeric mixture, preferably by precipitation of the R enantiomer, and subsequent acetylation of the optically pure intermediate.

    摘要翻译： 描述了使用D，L-丝氨酸作为起始原料合成Lacosamide的新方法，其中羟基的甲基化反应使用廉价的碱如NaOH和廉价的烷基化剂进行，无毒和非致癌， 如对甲苯磺酸甲酯; 选择性水解乙酰胺后，将R对映异构体与赖氨酰胺的外消旋混合物分离，用有机溶剂中的手性酸（HX *）进行外消旋混合物的成盐，非对映异构体混合物的拆分，优选通过沉淀R对映异构体， 和随后的光学纯中间体的乙酰化。