METHOD OF PRODUCING 2,5-DISUBSTITUTED 6-HYDROXYPYRIMIDIN-4(3H)-ONE Russian patent published in 2016 - IPC C07D239/54 

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing 2,5-disubstituted 6-hydroxypyrimidin-4(3H)-ones of formula I , where R₁=Me, R₂=H (2-methyl-6-hydroxypyrimidin-4(3H)-one); R₁=Me, R₂=Et (6-hydroxy-2-methyl-5-ethylpyrimidin-4(3H)-one); R₁=Me, R₂=Bu (5-butyl-6-hydroxy-2-methylpyrimidin-4(3H)-one); R₁=Me, R₂=Bz (5-benzyl-6-hydroxy-2-methylpyrimidin-4(3H)-one); R₁=Me, R₂=Ph (6-hydroxy-2-methyl-5-phenylpyrimidin-4(3H)-one); R₁=Ph, R₂=H (6-hydroxy-2-phenylpyrimidin-4(3H)-one); R₁=Me, R₂=Vin (5-vinyl-6-hydroxy-2-methylpyrimidin-4(3H)-one); R₁=4-ClPh, R₂=H (6-hydroxy-2-(4-chlorophenyl)pyrimidin-4(3H)-one); R₁=4-NO₂Ph, R₂=H (6-hydroxy-2-(4-nitrophenyl)pyrimidin-4(3H)-one); R₁=4-CH₃Ph, R₂=H (6-hydroxy-2-(4-tolyl)pyrimidin-4(3H)-one). Process is carried out in a medium of absolute benzene with reaction of substituted amidine, selected from: acetamidine, benzamidine, 4-chlorobenzamidine, 4-nitrobenzamidine, 4-methylbenzamidine, at a ratio of 1:1.5 with freshly prepared corresponding 2-substituted malonyl dichloride at a temperature of 50 °C for 1 hour with precipitation target pyrimidine.

EFFECT: invention increases output of product, reduces temperature and reduces reaction time.

1 cl, 4 tbl, 10 ex