| 摘要 |
Bicyclic cpds. of formula (I) and their acid addn. salts are new: (where R1 is H, 1-4C alkyl, cyclohexyl or benzyl. R is at least 4C alkyl, cyclohexyl, phenyl (opt. substd. by one or more halo or by one methyl, methoxy, hydroxy, cyano, nitro, trifluoromethyl, carboxy, ethoxycarbonyl, acetamido, methylsulphonyl, phenoxy, benzoyl, phenyl, alpha-hydroxybenzyl, cyclohexyl or carbamoyl), thienyl, pyridyl, naphthyl opt. substd. by methoxy, adamantyl or benzyl. n is 1-3 but cannot be 3 when R is phenyl substd. by carboxy, benzoyl or alpha-hydroxybenzyl. R1 cannot be benzyl when R is alpha-hydroxybenzyl-substd. phenyl). Also new are the intermediates (II), (IIa), (IIb), (IIc) and (V). (R' is as R but not phenyl substd. by carboxy or alpha-hydroxybenzyl. m is 1 or 2. R'"1 is as R1 but not H. R" is as R but not phenyl substd. by carboxy, alpha-hydroxybenzyl or benzoyl. R'1 is 1-4C alkyl, cyclohexyl or benzyl). (I) are useful as analgesics and can be administered orally, rectally or by injection. Most cpds. have acute intraperitoneal LD50 in mice over 300mg per kg. |
