SUBSTITUTED PHENYLACETYLENES SHOWING ABILITY TO INHIBIT SPECIFICALLY 5-LIPOXYGENASE ACTIVITY Russian patent published in 1994 - IPC

FIELD: organic chemistry. SUBSTANCE: product: substituted phenylacetylenes of the general formula R₂-C ≡ C-C₆H₃(m-R₁)(n-R₁), where one of radicals R₁ means hydrogen, and other one - a group of the general formula I, R₃, where R₄ -hydrogen, methyl or ethyl; R₂ - methyl or amino-group; R₅ means a) mono- or binucleus aromatic residue of the general formula II, (C₁-C₄), (C₁-C₄), R₆ or R₁, where means hydrogen, linear or branched alkyl-, alkoxy-, fluorine, chlorine or trifluoromethyl; n = 1,2 or 3, or b) mono- or binucleus heterocyclic residue containing sulfur, nitrogen or oxygen of the general formula III, , , or , where means hydrogen, chlorine or methyl. Reagent 1: compound of substituted phenylacetylene, in which radicals are at meta- and para-positions. Reagent 2: hydroxylamine. Reaction conditions: synthesized oxime is reduced with boron hydride, and acyl residue is added. Synthesized compounds are used in medicine since they can inhibit 5-lipoxygenase activity. EFFECT: improved method of synthesis. 3 tbl