4-HYDROXYBENZOPYRAN-2-ONE OR 4-HYDROXYCYCLOALKYL[B]BENZOPYRAN- -2-ONE AND, METHOD OF SYNTHESIS OF N-[3-[CYCLOPROPYL- -(5,6,7,8,9,10-HEXAHYDRO-4-HYDROXY-2-OXO-2H-CYCLOOCTA[B]- -PYRAN-3-YL)METHYL]PHENYL]-BENZENESULFONE Russian patent published in 1999 - IPC

FIELD: organic chemistry. SUBSTANCE: invention relates to 4-hydroxybenzopyran- -2-ones and 4-hydroxycycloalkyl[b]pyran-2-ones of the formula (I) and their sulfoneamide derivatives of the formula (XI) as inhibitors of HIV-proteinase. In formulas (I), (XI): R₁₀ and R₂ taken together mean formula (II) or (III) ; R₀ is H; R₁ is H, -OC_nH_2n+1, F, NH₂, -O--C_nH_2n-Het; R₂ is H, -OC_nH_2n+1,CF₃,-OC_nH_2nCH=CH₂ or -O-C_nH_2n-Het; or R₁ and R₂ taken together mean phenyl; or R₀ and R₂ taken together mean phenyl; R₃ is , diphenylethyl, diphenylethenyl, CH-C₃H₆-cycloalkyl)₂, 5,6,7,8-tetrahydro-5H-benzocyclo- -heptenyl, 1,2,3,4-tetrahydronaphthalenyl substituted with one or two -OC_nH_2n+1-groups or CH₃CH(CH₂-phenyl)₂ and other values. Method of synthesis of (XI) involves an interaction of compound of the formula (XII) with (XIII) in hydrocarbon solvent in the presence of trialkylamine at increased temperature in an organic solvent and synthesized amino-derivative (XV) is subjected for interaction with benzoyl sulfochloride. EFFECT: improved method of synthesis, enhanced efficiency of compounds. 24 cl, 67 dwg, 4 tbl, 486 ex