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    Process for the preparation of amino methyl cyclo alkane acetic acids
    1.
    发明授权
    Process for the preparation of amino methyl cyclo alkane acetic acids 有权
    制备氨基甲基环烷烃乙酸的方法

    公开(公告)号：US07635717B2

    公开(公告)日：2009-12-22

    申请号：US10535253

    申请日：2002-11-20

    申请人： Nagarajan Kuppuswamy ,  Sivaramakrishnan Hariharan ,  Arulselvan Mariadas

    发明人： Nagarajan Kuppuswamy ,  Sivaramakrishnan Hariharan ,  Arulselvan Mariadas

    IPC分类号： A61K31/195 ,  C07C229/32

    CPC分类号： C07C227/18 ,  C07C227/38 ,  C07C2601/14 ,  C07C229/28

    摘要： This invention relates to an improved process for the preparation of amino methyl cyclo alkane acetic acids. This invention particularly relates to an improved process for the preparation of gabapentin (which is chemically known as 1-aminomethyl-1-cyclohexaneacetic acid), which is a very well known agent useful for the treatment of epilepsy and other cerebral disorders. In the chemical series of 1-amino methyl cyclo alkane-1-acetic acids, Gabapentin, which is 1-amino methyl cyclo hexane-1-acetic acid has been developed as a drug having anti convulsive properties.

    摘要翻译： 本发明涉及一种制备氨基甲基环烷烃乙酸的改进方法。 本发明特别涉及用于制备加巴喷丁（其化学上称为1-氨基甲基-1-环己烷乙酸）的改进方法，其是用于治疗癫痫和其它脑病的非常熟知的药剂。 在1-氨基甲基环烷-1-乙酸的化学系列中，开发了作为1-氨基甲基环己烷-1-乙酸的加巴喷丁作为具有抗惊厥性质的药物。

    Process for the preparation of gabalactam
    3.
    发明授权
    Process for the preparation of gabalactam 有权
    制备日巴拉内酰胺的方法

    公开(公告)号：US07632953B2

    公开(公告)日：2009-12-15

    申请号：US10535278

    申请日：2002-11-20

    申请人： Nagarajan Kuppuswamy ,  Sivaramakrishnan Hariharan ,  Arulselvan Mariadas

    发明人： Nagarajan Kuppuswamy ,  Sivaramakrishnan Hariharan ,  Arulselvan Mariadas

    IPC分类号： C07D209/54 ,  A61K31/4015

    CPC分类号： C07D209/54

    摘要： The present invention provides an improved process for the preparation of gabalactam of formula 1 that includes preparing an aqueous solution of an alkali or alkaline earth metal hydroxide, adding bromine to the resulting solution to give an appropriate alkali or alkaline earth metal hypobromite; adding an amide of the formula 4 aging the resultant mixture; heating the mixture to a temperature in a range of 80 to 100 degrees C.; extracting with nonpolar solvent and distilling under reduced pressure to obtain gabalactam.

    摘要翻译： 本发明提供了制备式1的内巴豆的改进方法，其包括制备碱金属或碱土金属氢氧化物的水溶液，向所得溶液中加入溴，得到适当的碱金属或碱土金属次溴酸盐; 加入式4的酰胺使所得混合物老化; 将混合物加热至80至100℃的温度; 用非极性溶剂萃取，减压蒸馏得到日巴拉内酰胺。