申请人:Sterling Drug Inc.
公开号:US03976653A1
公开(公告)日:1976-08-24
1,2,3,4,4a,5,10,10a-octahydro-5-(Y.sup.3)-5-(Y.sup.4)-benzo[g]quinolines and 1,2,3,4,4a,9b-hexahydro-5-(Y.sup.3)-5-(Y.sup.4)-5H-indeno[1,2,b]pyridi nes wherein Y.sup.3 and Y.sup.4 are hydrogen, alkyl or phenyl, which are useful as antagonists of strong analgesics, are obtained by cyclizing derivatives of 2-(phenyl or benzyl)-.alpha.-(Y.sup.3)-.alpha.-(Y.sup.4)-3-piperidinemethanols. The latter are obtained from corresponding 3-piperidinecarboxylic acids.
1,2,3,4,4a,5,10,10a-八氢-5-(Y.sup.3)-5-(Y.sup.4)-苯并[g]喹啉和1,2,3,4,4a,9b-六氢-5-(Y.sup.3)-5-(Y.sup.4)-5H-吲哚[1,2,b]吡啶,其中Y.sup.3和Y.sup.4是氢、烷基或苯基,可用作强镇痛药的拮抗剂,通过环化2-(苯基或苄基)-.alpha.-(Y.sup.3)-.alpha.-(Y.sup.4)-3-哌嗪甲醇的衍生物得到。后者是从相应的3-哌嗪甲酸衍生物获得的。