Process for preparation of Irbesartan
    1.
    发明授权
    Process for preparation of Irbesartan 失效
    厄贝沙坦制备方法

    公开(公告)号:US07652147B2

    公开(公告)日:2010-01-26

    申请号:US11406919

    申请日:2006-04-19

    IPC分类号: C07D257/00 C07D403/00

    摘要: A process for the preparation of Irbesartan of formula (I) using the steps of: (i) reacting 4′ aminomethyl-2-cyano biphenyl of formula (VI) with 1-veleramido cyclopentane carboxylic acid of formula (V) in an organic solvent and in the presence of an acid, without activating the —COOH group of compound of formula (V) to give 1-(2′cyanobiphenyl-4-yl-methylaminocarbonyl)-1-pentanoylamino cyclopentane of formula (VII). converting the compound of formula (VII) obtained in step (i) to Irbesartan of formula (I) by reacting the compound of the formula (VII) with tributyl tin azide in o-xylene to give Irbesartan of formula (I).

    摘要翻译: 使用以下步骤制备式(I)的厄贝沙坦的方法:(i)使式(VI)的4'-氨基甲基-2-氰基联苯与式(V)的1-维拉酰氨基环戊烷羧酸在有机溶剂 并且在酸存在下,不活化式(Ⅴ)化合物的-COOH基,得到式(Ⅶ)的1-(2'-氰基联苯-4-基 - 甲基氨基羰基)-1-戊酰基氨基环戊烷。 通过使式(Ⅶ)化合物与叠氮化三丁基锡在邻二甲苯中反应,得到式(ⅰ)中得到的式(Ⅶ)化合物转化成式(I)所示的厄贝沙坦,得到式(I)的厄贝沙坦。