IMPROVED METHOD OF PRODUCING 4-(BENZIMIDAZOLYL METHYLAMINO)-BENZAMIDES AND SALTS THEREOF Russian patent published in 2012 - IPC C07D271/06 C07D401/12 C07D413/14 

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing optionally substituted 4-(benzimidazo-2-yl methylamino)benzamidine of formula (I) in which R¹ denotes a methyl group, R² denotes a R²¹NR²² group, where R²¹ denotes an ethyl group which is substituted with an ethoxycarbonyl group, and R²² denotes a pyridin-2-yl group, R³ denotes an n-hexyloxycarbonyl group, where at step (a) phenyldiamine of formula (II) where R¹ and R² assume values given for formula (I), which reacts with 2-[4-(1,2,4-oxadiazol-5-on-3-yl)phenylamino]acetic acid, to obtain a product of formula (III) where R¹ and R² assume values given for formula (I), which is hydrogenated at temperature from 30 to 60°C at hydrogen pressure from 1 to 10 bar, over palladium on activated charcoal (Pd/C) in a mixture of tetrahydrofuran and water, and then, without any preliminary extraction of the hydrogenation product, the obtained compound of formula (I), in which R³ denotes hydrogen, in the presence of potassium carbonate reacts with a compound of formula (IV) R³-X (IV), where R³ assumes values given for formula (I), and X denotes a suitable splitting group.

EFFECT: simple method of producing optionally substituted 4-(benzimidazo-2-yl methylamino)benzamidine.

3 cl, 9 ex