METHOD FOR OBTAINING ACYCLOXY-SUBSTITUTED BARBITURIC ACIDS Russian patent published in 2018 - IPC C07D239/62 

FIELD: chemistry.

SUBSTANCE: invention relates to a novel process for obtaining new derivatives of barbituric acid – acyloxy-substituted 1,3-dimethyl-2,4,6-trihydroxypyrimidines of general formula (I) Compounds can be used in medicine for producing medicaments, since they contain a pharmacophore portion of barbituric acid 2,4,6-trihydroxypyrimidine (2,4,6-pyrimidinetrione). In general formula (I) R = phenyl, substituted or unsubstituted benzyl; R₁ and R₂=Et either R₁+R₂=(CH₂)₂, (CH₂)₃ or (CH₂)₄. Method according to the invention consists in that the corresponding 1,3-dimethyl-2,4,6-trihydroxypyrimidine of general formula (II) (II) (III) is reacted with the corresponding malonyl peroxide of general formula (III) where R, R₁ and R₂ have the above meanings, in the presence of trifluoroethanol or hexafluoroisopropanol. Process is preferably carried out at a molar ratio of 1,3-dimethyl-2,4,6-trihydroxypyrimidine : malonyl peroxide : trifluoroethanol or hexafluoroisopropanol 1:1.1:19–28.

EFFECT: technical result of the proposed method is production of new barbituric acid derivatives in one step with a high yield of 81 to 90 %; the introduction of functional substituents in the 5-position gives the possibility for their further modification, and also allows to increase their solubility in water, and, consequently, to increase their bioavailability, and which can be used.

1 cl, 16 ex