FIELD: organic chemistry, chemical technology, pharmacy.
SUBSTANCE: invention relates to a method for preparing 6-substituted derivatives of 2-(alkylsulfanyl)-4(3H)-pyrimidinone of the general formula (I) that are used as intermediate products for synthesis of medicinal preparations and as independent medicinal preparations. In compounds of the formula (I),
R means C6H5CH2; R' means CH3, CH(CH3)C2H5, cyclo-C5H9, cyclo-C6H11; R means 2,6-F2C6H3CH2; R' means CH3, CH(CH3)C2H5, cyclo-C5H9, cyclo-C6H11; R means 2,6-Cl2C6H3CH2; R' means CH3, CH(CH3)C2H5, cyclo-C5H9, cyclo-C6H11; R means 1-C10H7CH2; R' means CH3, CH(CH3)C2H5, cyclo-C5H9, cyclo-C6H11; R means Ph2CH; R' means CH3, C2H5, CH(CH3)C2H5, cyclo-C5H9, C6H11. Method involves the following reactions. S-Alkylisothiourea hydrohalogen taken among the group: S-methylisothiourea hydroiodide, S-ethylisothiourea hydrobromide, S-sec.-butylisothiourea hydrobromide, S-cyclopentylisothiourea hydrobromide or S-cyclohexylisothiourea hydrobromide prepared into reactor directly (in situ) from thiourea and corresponding halogenalkane or sec.-butanol or cycloalkanol in the presence hydrobromic acid is subjected for interaction with 4-aryl-3-oxobutanoic acid methyl ester or 4,4-diaryl-3-oxobutanoic acid methyl ester in ethanol solution in the presence of potassium carbonate an aqueous solution wherein indicated methyl esters of acid are taken among the following group: 4-phenyl-3-oxobutanoic acid methyl ester, 4-(2,6-difluorophenyl)-3-oxobutanoic acid methyl ester, 4-(2,6-dichlorophenyl)-3-oxobutanoic acid methyl ester, 4-(1-naphthyl)-3-oxobutanoic acid methyl ester and 4,4-diphenyl-3-oxobutanoic acid methyl ester in the mole ratio 4-aryl-3-oxobutanoic acid methyl ester or 4,4-diaryl-3-oxobutanoic acid methyl ester : S-alkylisothiourea hydrohalogen : potassium carbonate = (1:1)-(3:1)-3, respectively, and the following isolation of the end product. Invention provides enhancing yield of claimed compounds, simplified process in preparing and isolating end products.
EFFECT: improved preparing method.
22 ex
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