发明名称 PROCESS FOR PRODUCING 9-ALKOXY- OR -ALLYLOXY-5-ALKYL- OR -ALKENYL-6,7-BENZOMORPHANE DERIVATIVES
摘要 Compounds of formula L <IMAGE> 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.
申请公布号 HU173039(B) 申请公布日期 1979.02.28
申请号 HU1975BI00514 申请日期 1975.04.17
申请人 BRISTOL MYERS CO,US 发明人 MONTZKA,THOMAS A.,US;MATISKELLA,JOHN D.,US
分类号 A61K31/435;A61K31/47;A61K31/485;A61P25/04;A61P25/30;C07C45/56;C07C45/68;C07C49/755;C07C231/00;C07D221/26;C07D401/12 主分类号 A61K31/435
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