METHOD FOR PRODUCING (1R,2S,5S)-N-[(1S)-1-CYANO-2-[(3S)-2-OXOPYRRROLIDIN-3-YL]ETHYL]-3-[(2S)-3,3- DIMETHYL-2-[(2,2,2-TRIFLUORACETYL)AMINO]BUTANOYL]-6,6-DIMETHYL-3-AZABICYCLO[3.1.0]HEXAN-2-CARBOXAMIDE Russian patent published in 2023 - IPC C07D209/52 C07D403/12 A61K31/403 

FIELD: medicine; pharmacology; pharmaceutical industry.

SUBSTANCE: group of inventions includes a method for producing (1R,2S,5S)-N-[(1S)-1-cyano-2-[(3S)-2-oxopyrrolidin-3-yl]ethyl]-3-[(2S)-3,3-dimethyl-2-[(2,2,2-trifluoroacetyl)amino]butanoyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane- 2-carboxamide (compound of formula (I)) and its use for batch chemical industrial production, semi-continuous industrial production or continuous industrial production, as well as a method for preparing an intermediate compound of formula (IV) intended for use in a method for producing a compound of formula (I). The process for preparing a compound of formula (I) includes the following steps: a) reaction of a compound of formula (V) or a salt thereof with a compound of formula (IV) using a compound of formula R₁O-CO-Cl, where R₁ is C₁-C₅ alkyl; C₁-C₅ alkyl substituted with halogen; phenyl; phenyl substituted with halogen, nitro or C₁-C₅ alkyl; benzyl substituted with halogen, nitro or C₁-C₅ alkyl in the presence of a base to give a compound of formula (VI); b) dehydration of the compound of formula (VI) using 2,4,6-trichloro-1,3,5-triazine to form a compound of formula (I). The process for preparing an intermediate compound of formula (IV) involves reaction of a compound of formula (II) with a compound of formula (III) in the presence of an aqueous solution of an alkali or alkaline earth metal hydrogen carbonate, where R is chlorine, bromine or fluorine.

EFFECT: improved method of obtaining, leading to an increase in the yield and chemical purity of the compound of formula (I).

39 cl, 1 tbl, 2 ex