PROCESS FOR THE PREPARATION OF 4-(BENZIMIDAZOLYLMETHYLAMINO)-BENZAMIDES AND THE SALTS THEREOF
    2.
    发明申请
    PROCESS FOR THE PREPARATION OF 4-(BENZIMIDAZOLYLMETHYLAMINO)-BENZAMIDES AND THE SALTS THEREOF 有权
    制备4-(苯并咪唑基甲基)氨基甲酸酯及其盐的方法

    公开(公告)号:US20100210845A1

    公开(公告)日:2010-08-19

    申请号:US12769718

    申请日:2010-04-29

    IPC分类号: C07D413/14 C07D401/12

    摘要: The invention relates to a process for preparing an optionally substituted 4-benzimidazol-2-ylmethylamino)-benzamidine, characterised in that (a) an optionally correspondingly substituted diaminobenzene is condensed with 2-[4-(1,2,4-oxadiazol-5-on-3-yl)-phenylamino]-acetic acid, (b) i) the product thus obtained is hydrogenated and ii) optionally the amidino group is carbonylated, without isolating the intermediate product of the hydrogenation beforehand; as well as a process for preparing a salt of an optionally substituted 4-(benzimidazol-2-ylmethylamino)-benzamidine, wherein (a) an optionally correspondingly substituted diaminobenzene is condensed with 2-[4-(1,2,4-oxadiazol-5-on-3-yl)-phenylamino]-acetic acid, (b) the product thus obtained is hydrogenated, and (c) i) optionally the amidino group is carbonylated and ii) without prior isolation of the intermediate product of the carbonylation the desired salt is isolated.

    摘要翻译: 本发明涉及制备任选取代的4-苯并咪唑-2-基甲基氨基) - 苄脒的方法,其特征在于(a)任选相应取代的二氨基苯与2- [4-(1,2,4-恶二唑-2-基) 5-苯基氨基] - 乙酸,(b)i)将如此获得的产物氢化,和ii)任选地将脒基羰基化,而不事先分离氢化的中间产物; 以及制备任选取代的4-(苯并咪唑-2-基甲基氨基) - 苄脒盐的方法,其中(a)任选相应取代的二氨基苯与2- [4-(1,2,4-恶二唑) -5-苯基氨基] - 乙酸,(b)将由此获得的产物氢化,和(c)i)任选地脒基被羰基化,和ii)不事先分离出中间产物 羰基化分离所需的盐。