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publicationDate 2012-07-10-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber RU-2455292-C2
titleOfInvention Improved method of producing 4-(benzimidazolyl methylamino)-benzamides and salts thereof
abstract FIELD: chemistry. n SUBSTANCE: invention relates to a method of producing optionally substituted 4-(benzimidazo-2-yl methylamino)benzamidine of formula (I) in which R 1 denotes a methyl group, R 2 denotes a R 21 NR 22 group, where R 21 denotes an ethyl group which is substituted with an ethoxycarbonyl group, and R 22 denotes a pyridin-2-yl group, R 3 denotes an n-hexyloxycarbonyl group, where at step (a) phenyldiamine of formula (II) where R 1 and R 2 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 R 1 and R 2 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 R 3 denotes hydrogen, in the presence of potassium carbonate reacts with a compound of formula (IV) R 3 -X (IV), where R 3 assumes values given for formula (I), and X denotes a suitable splitting group. n EFFECT: simple method of producing optionally substituted 4-(benzimidazo-2-yl methylamino)benzamidine. n 3 cl, 9 ex
priorityDate 2005-12-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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