4-METHYL-N-2,4-DIMETHYLPHENYL-6-(3-FLUOROPHENYL)-2-THYOXO-1,2,3,6-TETRAGYDROPYRIMIDINE-5-CARBOXAMIDE THAT HAS ANALGETIC ACTION Russian patent published in 2018 - IPC C07D239/40 A61P29/00 

Abstract RU 2653511 C2

FIELD: biochemistry.

SUBSTANCE: invention relates to a novel pyrimidine-4-methyl-N-2,4-dimethylphenyl-6-(3-fluorophenyl)-2-thioxo-1,2,3,6-tetrahydropyrimidine-5-carboxamide derivative of formula (1) . Compound has an analgesic effect, which suggests its use in medicine as an analgesic. Compound 1 is prepared by reacting a three-component condensation of 2,4-dimethylacetoacetanilide, 3-fluorobenzaldehyde and thiourea while maintaining the reagents at a temperature of 120–150 °C until the gas evolution ceases and the reaction mixture solidifies, after cooling, the residue is treated with ethanol. Claimed compound is a colorless crystalline substance with Tpl. 236–238 °C, soluble in dimethylformamide, acetic acid, when heated – in ethanol, stable during storage. LD50 of the compound when administered intraperitoneally to non-linear mice is > 5100 mg/kg.

EFFECT: activity of compound 1 surpasses the activity of metamizole sodium.

1 cl, 1 tbl

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RU 2 653 511 C2

Authors

Gejn Vladimir Leonidovich

Zamaraeva Tatyana Mikhajlovna

Buzmakova Nadezhda Albertovna

Syropyatov Boris Yakovlevich

Alikina Nataliya Viktorovna

Dates

2018-05-10Published

2015-07-29Filed