METHOD OF SYNTHESIS OF 5-LIPOXYGENASE INHIBITORS HAVING DIFFERENT HETEROCYCLIC SYSTEMS

摘要

FIELD: organic chemistry of heterocyclic compounds, biochemistry, pharmacy. SUBSTANCE: invention describes method of synthesis of compound (1.3.0) where is a group taken among the formulas (1.3.2) , (1.3.3) , (1.3.4) or (1.3.5) involving the formation of reactive mixture consisting of carboxamide of the formula (2.0.0) and the corresponding bicyclic N-heterocycle in aprotonic solvent in the presence of strong base in solid form taken among the group including sodium hydroxide and potassium hydroxide and, optionally, in the presence of catalytical amount of cesium carbonate, Cs₂CO₃, or catalyst of interphase transfer followed by heating the indicated reactive mixture under nitrogen atmosphere and yielding the end compound. Also, invention describes method of synthesis of one of particular compound and method of synthesis of compound mesilate salt. Synthesized compounds can be useful for treatment of patients with inflammatory diseases and allergy. EFFECT: improved method of synthesis of known and new inhibitors of 5-lipoxygenase, valuable medicinal properties of compounds. 8 cl, 3 tbl, 18 ex