发明名称 PROCESS FOR THE PREPARATION OF 4-(BENZIMIDAZOLYLMETHYLAMINO)-BENZAMIDES AND THE SALTS THEREOF
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.
申请公布号 US2010210845(A1) 申请公布日期 2010.08.19
申请号 US20100769718 申请日期 2010.04.29
申请人 BOERINGER INGELHEIM INTERNATIONAL GMBH 发明人 ZERBAN GEORG;HAUSHERR ARNDT;SCHLARB KERSTIN;HAMM RAINER;KOCH GUNTER;WEYELL BJOEM;SCHMITT HEINZ-PETER
分类号 C07D413/14;C07D401/12 主分类号 C07D413/14
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