2-CYANO-3-HYDROXYPROPENEAMIDES, METHODS OF THEIR SYNTHESIS AND A PHARMACEUTICAL COMPOSITION BASED ON SAID Russian patent published in 1999 - IPC

Abstract RU 2126387 C1

FIELD: organic chemistry and technology, pharmacy. SUBSTANCE: invention relates to 2-cyano-3-hydroxypropeneamides of the formula (I) where each of A, B and E means =CH-group or nitrogen atom; R is C3-C6-cycloalkyl; R1 is hydrogen; R2 and R3 are similar or distinct - hydrogen, C1-C6-alkyl, trifluoromethyl, halogen, nitro-group. Invention relates to also methods of synthesis of compounds of the formula (I). The 1-st method: compound of the formula (II) is subjected for interaction with sodium hydride and then with functional derivatives of an acid of the formula Hal-C(O)-RA where Hal is halogen atom; RA has values R or they are R-protected radical. The synthesized compound of the formula (IA) is isolated after protecting group removal if necessary. The 2-d method: compounds of the formula (IV) are subjected for interaction with a strong base. Invention relates to a pharmaceutical composition containing a compound of the formula (I) taken at effective amount and exhibiting an antiinflammatory activity. EFFECT: improved methods of synthesis, enhanced effectiveness of compounds. 9 cl, 2 tbl, 10 ex

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RU 2 126 387 C1

Authors

Ehlizabet Ann Kjuo

Dates

1999-02-20Published

1994-01-04Filed