CRYSTAL OF 5-HYDROXY-1N-IMIDAZOL-4-CARBOXAMIDE& 3/4 HYDRATE, PRODUCTION METHOD AND CRYSTAL OF 5-HYDROXY-1N-IMIDAZOL-4-CARBOXAMIDE HYDRATE Russian patent published in 2017 - IPC C07D233/90 A61K31/4164 A61P35/00 

Abstract RU 2630682 C2

FIELD: chemistry.

SUBSTANCE: invention relates to the method of producing 5-hydroxy-1N-imidazole-4-carboxamide⋅3/4 hydrate comprising the reaction of 2-aminomalonamide with a compound represented by the following formula

in the presence of alcohols and in the presence of a carboxylic acid, which includes formic acid or oxalic acid or in the presence of alcohols and in the absence of a mineral acid and in the absence of sulphonic acid, to produce 5-hydroxy-1N-imidazole-4-carboxamide, where in formula [1], each R is independently C1-3 alkyl group; the reaction of the resulting 5-hydroxy-1N-imidazole-4-carboxamide with an acidic hydrochloric acid compound to give the hydrate of the acid salt of 5-hydroxy-1N-imidazole-4-carboxamide; and the reaction of the resulting hydrate of the acid salt of 5-hydroxy-1N-imidazole-4-carboxamide with, at least, one salt selected from the group consisting of sodium acetate, sodium formate, potassium formate and sodium malate in the presence of hydrochloric acid as acidic solvent, at the temperature from room temperature of up to 60°C for 1 minute to 24 hours, to produce 5-hydroxy-1N-imidazole-4-carboxamide 3/4⋅ hydrate.

EFFECT: method for producing a compound has been developed, characterized by a high yield of the target compound and purity, and stability.

6 cl, 16 dwg, 8 tbl, 32 ex

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RU 2 630 682 C2

Authors

Fudzimoto Tajsuke

Khasimoto Tomokhiro

Khayasi Katsuyuki

Tanaka Tomoyuki

Dates

2017-09-12Published

2012-09-28Filed