| abstract |
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): R 10 and R 2 taken together mean formula (II) or (III) ; R 0 is H; R 1 is H, -OC n H 2n+1 , F, NH 2 , -O--C n H 2n -Het; R 2 is H, -OC n H 2n+1 ,CF 3 ,-OC n H 2n CH=CH 2 or -O-C n H 2n -Het; or R 1 and R 2 taken together mean phenyl; or R 0 and R 2 taken together mean phenyl; R 3 is , diphenylethyl, diphenylethenyl, CH-C 3 H 6 -cycloalkyl) 2 , 5,6,7,8-tetrahydro-5H-benzocyclo- -heptenyl, 1,2,3,4-tetrahydronaphthalenyl substituted with one or two -OC n H 2n+1 -groups or CH 3 CH(CH 2 -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 |