6,6-DIMETHYL-8-OXO-5,6,8,9-TETRAHYDROBENZO[F]-PYRROLO[2,1-ALPHA]ISOQUINOLINE-9-SPIRO-2-(3-AROYL-4-HYDROXY-1-O-HYDROXYPHENYL-5-OXO-2,5-DIHYDRO-1H-PYRROLES) AND 6,6-DIMETHYL-8-OXO-5,6,8,9-TETRAHYDROBENZO[F]PYRROLO[2,1-ALPHA]ISOQUINOLINE-9-SPIRO-2-(3-BENZOYL-4-HYDROXY-1-O-HYDROXYPHENYL-5-OXO-2,5-DIHYDRIO-1H-PYRROLE) ELICITING ANALGESIC ACTIVITY AND METHOD FOR THEIR PREPARING

摘要

FIELD: organic chemistry, chemical technology, medicine. ^ SUBSTANCE: invention describes 6,6-dimethyl-8-oxo-5,6,8,9-tetrahydrobenzo[f]pyrrolo[2,1-alpha]isoquinoline-9-spiro-2-(3-aroyl-4-hydroxy-1-o-hydroxyphenyl-5-oxo-2,5-dihydro-7H-pyrroles) and 6,6-dimethyl-8-oxo-5,6,8,9-tetrahydrobenzo[f]pyrrolo[2,1-alpha]isoquinoline-9-spiro-2-(3-benzoyl-4-hydroxy-1-o-hydroxyphenyl-5-oxo-2,5-dihydro-1H-pyrrole) of the formula (I) (a, b, c) wherein Ar means C6H5 (a); p-C6H4OMe (b); p-C6H4Br (c) eliciting analgesic activity and related to substituted 13-aza-analogs of steroids, and to a method for their synthesis. Invention provides the development of a simple method of synthesis of 6,6-dimethyl-8-oxo-5,6,8,9-tetrahydrobenzo[f]pyrrolo[2,1-alpha]isoquinoline-9-spiro-2-(3-aroyl-4-hydroxy-1-o-hydroxyphenyl-5-oxo-2,5-dihydro-1H-pyrroles) related to 13-azagonanes - heterocyclic analogs of steroid comprising a spiro-heterocyclic substitute at position 16 of tetracyclic system among them compound 6,6-dimethyl-8-oxo-5,6,8,9-tetrahydrobenzo[f]pyrrolo[2,1-alpha]isoquinoline-9-spiro-2-(3-benzoyl-4-hydroxy-1-o-hydroxyphenyl-5-oxo-2,5-dihydro-1H-pyrrole) elicits analgesic activity and these compounds have not been described. The proposed reaction represents a novel approach to synthesis of heterocyclic analogs of steroids. ^ EFFECT: improved method of synthesis, valuable medicinal property of compound. ^ 2 tbl, 3 ex