METHOD OF PRODUCING HETEROARYL PYRIMIDONE DERIVATIVE AND INTERMEDIATE COMPOUND OF HETEROARYL PYRIMIDONE DERIVATIVE Russian patent published in 2021 - IPC C07D487/04 C07D513/04 

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing a compound of formula (I), which includes a step of reacting a compound of formula (III) with a compound of formula (II) to obtain a compound of formula (I), where G is C, D and E are N, or D is C, and E is S; R₁ is selected from a group consisting of C_1-4 alkyl, phenyl and pyridazinyl; R₂ is C_1-4 alkyl, where C_1-4 alkyl is further substituted with one substitute selected from a group consisting of phenyl, where phenyl is further substituted with one or more substitutes selected from a group consisting of halogen; R₃ is C_1-4 alkyl; R₄ is selected from a group consisting of hydrogen and phenyl; Ra is C_1-4 alkyl; m equals 0; and n equals 1; reaction solvent is tetrahydrofuran, the reagent contains N,N-diisopropylethylamine, and the reaction solution is stirred at 15–40 °C for 16–18 hours, wherein the method further includes the following steps: reacting a compound of formula (VI) with a compound of formula (V) to obtain a compound of formula (IV), then a compound of formula (III) is obtained from a compound of formula (IV), where compound of formula (VI) is monometallic alkoxide or bimetallic alkoxide, M is selected from sodium ion; where for reaction of conversion of compound (VI) to compound (IV) with reaction solvent is N,N-dimethylformamide, reagent contains 2,6-difluorochlorobenzyl and N,N-diisopropylethylamine, and the reaction solution is heated to 80–110 °C and stirred for 1–3 hours, where for reaction of converting compound (IV) into compound (III) reaction solvent is ethanol, reagent contains hydrochloric acid and tin chloride dihydrate, and reaction solution is stirred at 15–40 °C for 1–3.5 hours, wherein method further includes a step of producing compound of formula (VI) from compound of formula (VII), where R^b is alkyl, the reaction solvent is methanol, the reagent contains sodium methoxide and the reaction solution is stirred at 30 °C for about 15 hours. Invention also relates to an intermediate compound of formula (VI) and a method for production thereof.

EFFECT: technical result is a novel method of producing a compound of formula (I) with high output, which can be used in medicine.

9 cl, 3 ex