METHOD FOR PRODUCING MONOSUBSTITUTED DERIVATIVES OF URACIL Russian patent published in 2018 - IPC C07D239/54 C07D239/553 

FIELD: chemistry.

SUBSTANCE: invention relates to a novel process for the preparation of N¹-substituted derivatives of uracil, which have a broad spectrum of biological activity, and can, for example, find application as antitumor medication. Process for the preparation of N¹monosubstituted derivatives of uracil or quinazoline-2,4-dione consists in the alkylation of a 1,3-dibenzoyl derivative of uracil or quinazoline-2,4-dione of general formula , where: R¹=H, CH₃, F or Br; R²=H or CH₃; R¹+R²=CH=CH-CH=CH, halide alkyl or alcohol toluene sulfonate in a polar aprotic solvent medium in an anhydrous medium in the presence of a base, followed by the addition of a concentrated aqueous solution of the base to the resulting alkylation product.

EFFECT: process allows to reach high regioselectivity of alkylation and increase in the yield of the target products to 59–89 %.

1 cl, 15 ex