E-2-ARYL-2-TRIFLUOROMETHYL-1-NITRO-CYCLOPROPANES AND A METHOD FOR PRODUCTION THEREOF Russian patent published in 2019 - IPC C07C13/04 C07C22/08 C07D213/16 A61K31/04 A61K31/75 A61P35/00 

Abstract RU 2699654 C1

FIELD: chemistry.

SUBSTANCE: invention relates to E-2-aryl-2-trifluoromethyl-1-nitro-cyclopropane of general formula I, where X=C, R=R1=H; X=C, R=Cl, R1=H; X=C, R=R1=Cl; X=C, R=Br, R1=H; X=C, R=R1=Br; X=C, R=C1-C3-alkyl, R1=H; X=C, R=NO2, R1=H; X=C, R=CO2Alk, R1=H; X=C, R=CF3, R1=H; X=C, R=OMe, R1=H; X=C, R=R1=OMe; X=C, R=F, R1=H; X=C, R-R1=-OCH2O-; X=N, R=R1=H. Also disclosed is a method of producing compounds I, consisting in batch addition of 4-15-fold molar excess of bromonitromethane and inorganic (preferably potassium carbonate) or organic (preferably 1,1-dimethyl-1,4,5,6-tetrahydropyrimidine) base to a solution of the corresponding α-(trifluoromethyl)styrene in a polar solvent, preferably dimethylsulphoxide (in case of an inorganic base) and 1,1,3,3-tetramethyl urea or N,N-dimethylformamide (in the case of an organic base) at room temperature.

EFFECT: obtaining novel compounds which can be used in medicine as anticancer agents for rectal cancer cells and human myelogenous leukemia.

7 cl, 1 tbl, 14 ex

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RU 2 699 654 C1

Authors

Golubev Aleksandr Sergeevich

Gorfinkel Sofya Mikhajlovna

Markova Alina Aleksandrovna

Suponitskij Kirill Yurevich

Peregudov Aleksandr Sergeevich

Strelkova Tatyana Vasilevna

Ostapchuk Petr Nikolaevich

Kagramanov Nikolaj Dmitrievich

Chkanikov Nikolaj Dmitrievich

Dates

2019-09-09Published

2019-04-26Filed