5-ARYL-4-FLUOROISOXAZOLES AND A METHOD FOR PRODUCTION THEREOF Russian patent published in 2019 - IPC C07D261/10 C07D261/18 A61P35/00 

Abstract RU 2708456 C1

FIELD: chemistry.

SUBSTANCE: invention relates to derivatives of 4-fluoroisoxazoles of general formula (I), where R1 is selected from CN3, CN3O, Cl, Br, F, H, and R2 is selected from CN3, Br, H. 4-fluoroisoazoles derivatives of formula (I) are obtained by aromatization of 5-aryl-4-bromo-4-fluoro-oxazolines of general formula (II), where R1 is CN3, CN3O, Cl, Br, F, H, and R2 is CN3, Br, H, by elimination of hydrogen bromide in the presence of a dehydrobromating agent in a polar solvent in the temperature range of 60–70 °C for 3–5 hours. Three-fold molar excess of a dehydrobromating agent is used, which is represented by silver salts or mercury salts or nitrosonium salts. Polar solvents used are ethanol or nitromethane.

EFFECT: as result, 4-fluoroisoxazole derivatives having antiproliferative action.

4 cl, 8 ex

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RU 2 708 456 C1

Authors

Bondarenko Oksana Borisovna

Komarov Arsenij Igorevich

Zyk Nikolaj Vasilevich

Dates

2019-12-09Published

2018-07-17Filed