FIELD: chemistry.
SUBSTANCE: invention relates to an improved method of producing 1-(w-hydroxyalkyl)uracils, which can be used in pharmaceutical industry as intermediate products in synthesis of medicinal compounds. Method consists in that uracil is subjected to silylation with excess of hexamethyldisilazane in presence of trimethylchlorosilane, obtained 2,4-bis-[(trimethylsilyl)oxy]pyrimidine is alkylated with subsequent cooling and treatment with 5 wt% with aqueous solution of sodium pyrosulphite and tetrahydro silvane. Then organic phase is separated by removal of solvent, evaporation to dryness at low pressure and alkaline hydrolysis of obtained product with boiling 5M solution of potassium hydroxide in 95 wt% ethanol with further removal of solvent, dissolution of residue in water and saturation of mixture with carbon dioxide. Extraction of the end product is carried out with tetrahydrosilvano with removal of water and evaporation of the solvent.
EFFECT: method increases output of end products to 57–72 % and simplifies the method by avoiding column chromatography.
1 cl, 5 ex
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Authors
Dates
2019-08-20—Published
2019-04-26—Filed