Improvements in or relating to isoquinolo[2,1-d]benzo[1,4]diazepine derivatives

摘要

Racemic and optically active compounds of the general formula (in which R represents a hydrogen atom or C1- 4 alkyl radical) and their acid addition salts are prepared by subjecting a compound of the formula to intramolecular ring closure, optionally followed by salt formation and/or resolution. The racemic and optically active starting materials are prepared by autoclaving I-(21 - chloro - 51 - nitrophenyl) - 3,4 - dihydroisoquinoline with RNH2 in the presence of cuprous chloride and copper powder, reducing the resulting compound of the formula with sodium borohydride and, if desired, resolving the product of the formula heating the racemate or optically active isomer with a C1- 4 alkyl bromoacetate or chloroacetate and saponifying the resulting compound of the formula (in which R1 represents a C1- 4 alkyl radical). The preparation of N-(b -phenethyl)-2-chloro-5-nitrobenzamide and 1-(21-chloro-51-nitrophenyl) -3,4-dihydroisoquinoline is described. Some of the compounds of the invention may be used as sedatives, sedative-hypnotics, tranquillizers, muscle relaxants, anticonvulsants and for the relief of anxiety, some are hypotensive agents and some are anti-inflammatory agents. They may be administered in the form of pharmaceutical preparations containing them together with a carrier.