BISULFATE OF JANUS KINAZE (JAK) INHIBITOR AND METHOD FOR ITS PREPARATION Russian patent published in 2018 - IPC C07D487/04 A61K31/519 A61P19/02 A61P29/00 

FIELD: chemistry.

SUBSTANCE: invention relates to bisulfate (3aR,5s,6aS)-N-(3-methoxy-1,2,4-thiadiazol-5-yl)-5-(methyl(7H-pyrrolo[2,3-d]pyrimidine-4-yl)amino)hexahydrocyclopenta[c]pyrrol-2(1H)-carboxamide of formula (I). Stoichiometric ratio of (3aR,5s,6aS)-N-(3-methoxy-1,2,4-thiadiazol-5-yl)-5-(methyl(7H-pyrrolo[2,3-d]pyrimidine-4-yl)amino)-hexahydrocyclopenta[c]pyrrole-2(1H)-carboxamide (compound IV) to sulfuric acid is 1:1. In the method, the process for the preparation of a compound according to the invention comprises a step of forming a salt of a compound of formula (IV) and sulfuric acid, wherein the salt formation reaction is carried out in a solvent and the solvent is a mixed solvent of halogenalkanes and alcohols having a number of carbon atoms, less than or equal to 3, preferably a mixed solvent of dichloromethane and methanol. Further, the reaction temperature for the salt formation reaction is from 10 to 30 °C, and the reaction time is from 0.5 to 4 hours. ,

EFFECT: bisulfate (3aR,5s,6aS)-N-(3-methoxy-1,2,4-thiadiazol-5-yl)-5-(methyl(7H-pyrrolo[2,3-d]pyrimidine-4-yl)amino)hexahydrocyclopenta[s]pyrrole-2(1H)-carboxamide of formula (I) has an inhibition activity of Janus kinase and is intended for the preparation of a medication for the treatment of rheumatism and rheumatoid arthritis.

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