PROCESS FOR THE PREPARATION OF GABAPENTIN HYDROCHLORIDE
    85.
    发明公开
    PROCESS FOR THE PREPARATION OF GABAPENTIN HYDROCHLORIDE 有权
    VERFAHREN ZUR HERSTELLUNG VON GABAPENTINHYDROCHLORID

    公开(公告)号:EP1939170A1

    公开(公告)日:2008-07-02

    申请号:EP06722414.7

    申请日:2006-04-28

    摘要: A process for preparation of gabapentin hydrochloride by converting 1,5-dicyano-2,4-dioxo-3-azaspiro[5,5]-undecane into 1,5-diaminoformyl-2,4-dioxo-3-azaspiro[5,5]-undecane at a temperature of 65°C to 85°C in the presence of a strong acid, and then carrying out Hofmann rearrangement under an alkaline condition. The starting material of the process is readily available. The process is simple, and can reduce the purification procedure of intermediates, reduce production cost, and obtain product with higher purity.

    摘要翻译: 通过将1,5-二氰基-2,4-二氧代-3-氮杂螺[5,5] - 十一烷转化为1,5-二氨基甲酰基-2,4-二氧代-3-氮杂螺[5, 5] - 十一碳烷,在强酸存在下,在65℃〜85℃的温度下进行,然后在碱性条件下进行霍夫曼重排。 该方法的起始材料是容易获得的。 该工艺简单,可以减少中间体的纯化程序,降低生产成本,获得更高纯度的产品。