Improved process for the preparation of the salts of...

C - Chemistry – Metallurgy – 07 – D

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C07D 235/14 (2006.01)

Patent

CA 2632310

The invention relates to a process for preparing a salt of 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, ii) optionally the amidino group is carbonylated, without isolating the intermediate product of the hydrogenation beforehand and iii) without prior isolation of the intermediate product of the carbonylation the desired salt is isolated.

L'invention concerne un procédé de préparation d'un sel de 4-benzimidazol-2-ylmethylamino)-benzamidine éventuellement substituée, caractérisé en ce que : (a) un diaminobenzène éventuellement substitué de manière correspondante est condensé avec 2-[4-(1,2,4-oxadiazol-5-on-3-yl)-phénylamino]-acide acétique ; et (b) i) le produit ainsi obtenu est hydrogéné, ii) éventuellement, le groupe amidino est carbonylé, sans isoler au préalable le produit intermédiaire de l'hydrogénation et iii) le sel désiré est isolé, sans isoler au préalable le produit intermédiaire de la carbonylation.

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