METHOD OF SYNTHESIS OF DERIVATIVE OF 8-CYCLO-PENTYL-6-ETHYL-3- (SUBSTITUTED)-5,8-DIHYDRO-4H-1,2,3A,7,8-PENTAAZA-AC-INDACENE (VARIANTS) AND INTERMEDIATE COMPOUNDS Russian patent published in 2002 - IPC

FIELD: organic chemistry, chemical technology. SUBSTANCE: invention describes the improved method of synthesis (and its variants) of derivatives of 8-cyclopentyl-6- ethyl-3-(substituted)-5,8-dihydro-4H-1,2,3a,7,8-pentaaza-aca-indacene of the formula (1.0.0) and its pharmaceutically acceptable salts where R¹ means (C₁-C₆)-alkyl or saturated or unsaturated (C₄-C₇)-heterocyclyl- group comprising one S-atom being the above indicated alkyl or heterocyclic group is optionally substituted with from 1 to 3 substitutes taken among (C₁-C₂)-alkyl, trifluoromethyl and halogen atom. The synthesis is performed from γ-caprolactone and n-methoxybenzylamine by the multistage synthesis through novel intermediate compounds of the formulas (8.1.0), (8.1.1) and (10.0.0). The end product synthesized by the described method is an inhibitor of phosphodiesterase type IV (PDE4) and secretion of tumor necrosis factor (TNF) that can be used in treatment of asthma, bronchitis, allergic rhinitis, psoriasis, dermatitis and other inflammatory, allergic and immunological diseases. EFFECT: improved method of synthesis, valuable medicinal properties. 7 cl, 1 tbl