METHOD OF PREPARING BENZOMORPHANES OR THEIR SALTS OR RACEMIC MIXTURE OR THEIR OPTICAL ISOMERS

摘要

Compounds of formula L wherein the substituents are defined in Claim 1, are prepared from corresponding 9 alpha -hydroxy compounds, in which the 2'-hydroxy group and the amino group are protected, by treatment with a strong base and subsequent alkylation to give a 9-OR<5> compound or by treatment of the blocked compound with a diazo(lower)alkane or tri(lower)alkyloxonium fluoroborate and subsequent alkylation, resulting in 9-OR<5>-substituted compounds. After cleaving off the protective groups and conversion to the 2'-OR<2> and 2-R<1> group, the compounds L are obtained. Compounds L with R<2>=H are converted to compounds with R<2>=lower alkyl by etherification. The compounds prepared are used as analgesics and/or as antagonists of narcotics and are non-addictive.