申请人:Bristol-Myers Company
公开号:US03931188A1
公开(公告)日:1976-01-06
Compounds having the formula ##SPC1## In which R is cyclopropyl or cyclobutyl have been designated 3-hydroxy-17-substituted-5,6-benzomorphinans. The compounds possess potent narcotic agonist and/or antagonist activity. In particular, the compounds 3-hydroxy-17-cyclopropylmethyl-5,6-benzomorphinan and 3-hydroxy-17-cyclobutylmethyl-5,6-benzomorphinan have been found to possess both activities. These compounds are prepared by total synthesis and are not derived from opium alkaloids.
化合物的化学式为##SPC1##其中R为环丙基或环丁基,已被指定为3-羟基-17-取代-5,6-苯并吗啡烷。这些化合物具有强效的麻醉受体激动剂和/或拮抗剂活性。特别地,化合物3-羟基-17-环丙基甲基-5,6-苯并吗啡烷和3-羟基-17-环丁基甲基-5,6-苯并吗啡烷已被发现具有这两种活性。这些化合物是通过全合成而制备的,而不是来源于鸦片生物碱。