Tetra:hydro-6-oxo-2,8a-methano-di:benzazocine derivs. - with central nervous, esp. analgesic and sedative, activity

摘要

(A) Dibenzazocine derivs. of formula (III) and their pharmaceutically acceptable salts are new. In (III), R1'= OH, or 1-3C alkoxy, R2' = H or 1-3c alkoxy, R3' = 1-3C alkoxy, R5' = H, 1-3C alkyl, is not >5C alkenyl, lower cycloalkylalkyl, or phenethyl (opt. ring substd. by >=1 lower alkoxy), R1' + R2' may also be methylenedioxy). (B) prodn. of cpds. (I) or their N-substd. derivs. comprises oxidative cyclisation of isoquinolines (II) or their N-substd. derivs. In the formulae, R1=OH or lower alkoxy and R2=H or lower alkoxy, or R1+R2 = lower alkylenedioxy, R3 = lower alkoxy or benzyloxy, R4 = lower alkoxy. (III) have CNS, esp. analgesic and sedative, activity. Individual doses are 25-100 mg and typical cpds. have LD50 (intragastral in mice) >=0.4 g/kg.