| 摘要 |
organic chemistry, chemical technology, pharmacy. SUBSTANCE: invention relates to novel 6-dimethylaminomethyl-1-phenylcyclohexane compounds of the general formula (I) as bases or their physiologically acceptable salts eliciting analgetic activity and designated for preparing a pharmaceutical composition and to methods of their synthesis. In general formula (I) radicals have the following values: R1 means H, OH, Cl or F; R2 and R3 are identical or different and mean H, C1-C4-alkyl, CF3, OH, OCH2-C6H5, O-C1-C4-alkyl under condition that at least one of radicals R2 or R3 means H; R4 means H, CH3, CO-(OC1-C5-alkyl), CO-NH-C6H4-C1-C3-alkyl, CO-C6H4-R5, CO-C1-C5-alkyl, CO-CHR6-NHR7 or unsubstituted pyridyl or phenyl group or which are substituted with C1-C4-alkyl; R5 means OC(O)-C1-C3-alkyl in orthoposition or CH2-N(R8)2 in meta- or para-position being both radicals R8 in common with N-atom mean 4-morpholine radical; and R6,R7 are identical or different and mean H or C1-C6-alkyl under condition that if both radicals R2 and R3 mean H then R4 is not CH3/ if R1 means H, OH or Cl; either R4 is not H if R1 means OH. Invention describes also different methods of synthesis of compounds of the formula (I). For example, for synthesis of compounds where R1 means OH dimethytlaminoketon of the formula (II) is subjected for interaction with organometallic compound of the formula (III) or dimethylaminoketon with spirocyclic acetal group of the formula (V) is subjected for interaction with organometallic compound of the formula (III) to yield the compound of the formula (VI) and the latter is converted to the keton compound (VIII) by deacetylation followed by reduction with alkaline metal complex hydride to the compound of the formula (I) which is converted to alkaline metal salt and then to the corresponding O-alkyl- or O-benzyl derivative. Invention describes also methods of synthesis of compounds where R1 means H or compounds where R1 means F. EFFECT: new compounds indicated above, improved methods of synthesis. 11 cl, 1 tbl
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