DERIVATIVES OF 2-CYANO-3-HYDROXYENAMIDES, METHOD FOR THEIR PRODUCTION, PHARMACEUTICAL COMPOSITION ON THEIR BASE
FIELD: organic chemistry; production of pharmaceutical compositions. SUBSTANCE: derivatives of 2-cyano-3-hydroxyenamides have formula I where R1 is group where R13-R15 are hydrogen atoms or C1-C3-alkyl; n= 1, 2, 3; R2 is hydrogen atom; R3-R7 are hydrogen atoms, nitro- or cyano group, halogen atom, C...
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Zusammenfassung: | FIELD: organic chemistry; production of pharmaceutical compositions. SUBSTANCE: derivatives of 2-cyano-3-hydroxyenamides have formula I where R1 is group where R13-R15 are hydrogen atoms or C1-C3-alkyl; n= 1, 2, 3; R2 is hydrogen atom; R3-R7 are hydrogen atoms, nitro- or cyano group, halogen atom, C1-C3-alkyl, group having formula -(CH2)m-CF3 or -O-(CH2)mCF3 or S-(CH2)m-CF3 where m=0 or R3-R7 are group having formula where R8-R12 are hydrogen atoms, halogen, CF3. Compounds having formula I are prepared by interaction of compound having formula II with sodium hydride, the process is carried out in the presence of catalyst. Then interaction with compound having formula IIIa Hal-C(=O)-RA (where RA is R1-radical being protected) takes place. Compound having formula I where R1 is (CH2)n,R17)C=C(R14,R15) group is prepared by interaction of compound IVa with compound VI (CXH2)n-1(R13)C=C(R14,R15). Compound having formula I is used as active ingredient for pharmaceutical composition, its quantity being within definite ranges. Pharmaceutical composition comprises also pharmaceutical acceptable diluents, carrier and/or excepients, composition has antiinflammatory action. EFFECT: improved quality of product, improved efficiency. 12 cl, 2 tbl |
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