2-HETARYL-SUBSTITUTED OF 1,3-TROPOLONE, METHOD FOR THEIR PREPARING (VARIANTS) AND PHARMACEUTICAL COMPOSITION WITH ANTIBACTERIAL EFFECT Russian patent published in 2008 - IPC C07D215/14 C07D401/04 C07D239/30 C07D213/30 A61K31/4453 A61P17/00 C07D215/18 C07D403/04 C07D239/42 C07D213/61 A61K31/5375 C07D215/44 C07D413/04 C07D241/16 C07D213/74 A61K31/498 C07D241/44 C07D221/06 C07D241/20 A61K31/47 A61P31/00 

Abstract RU 2314295 C2

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to 2-hetaryl-substituted derivatives of 1,2-tropolones of the general formula (Ia): wherein R1 and R2 mean (C1-C6)-alkyl; R3 means hydrogen atom, (C1-C6)-alkyl, nitro-group; Het means six-membered nitrogen heterocycle condensed with one or two benzyl rings that can be substituted with substitutes chosen from group comprising halogen atom, nitro-group, (C1-C6)-alkyl, oxy-(C1-C6)-alkyl, secondary amino-group chosen from anilino-, substituted anilino-, hydroxyethylamino-group, or tertiary amino-group chosen from morpholino-, piperidino-, piperazino-group, 1H-1-imidazolyl. Also, invention relates to a method for synthesis of 2-hetaryl-substituted derivatives of 1,3-tropolone. Method involves condensation of benzoquinones-1,2 with 2-methylheterocycles at heating in the presence of acetic acid taken in the amount providing its role as both a catalyst and a solvent. Also, invention relates to a pharmaceutical composition with antibacterial effect based on 2-hetaryl-substituted derivatives of 1,3-tropolone.

EFFECT: improved method of synthesis, valuable medicinal properties of compounds and pharmaceutical composition.

9 cl, 5 tbl, 3 ex

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RU 2 314 295 C2

Authors

Komissarov Vitalij Nikolaevich

Sajapin Jurij Anatol'Evich

Minkin Vladimir Isaakovich

Dates

2008-01-10Published

2006-03-01Filed