process for the production of new 1,3,4,14btetrahydro - 2h, 10am - pyrazino (1.2 (a) pyrrolo (2.1) (1.4), benzodiazepines, their salts and optical isomers

摘要

1. A 1,3,4,14b-tetrahydro-2H, 10H-pyrazino[1,2-a]pyrrolo[2,1-c][1,4]benzodiazepine of the general formula I see diagramm : EP0001585,P19,F1 wherein each of R1 , R3 and R4 is hydrogen or lower alkyl ; R2 is hydrogen, lower alkyl or higher alkyl, lower alkenyl, lower alkynyl, cycloalkyl or cycloalkenyl, each containing 3 to 7 ring members, or (cycloalkyl, hydroxy, amino, mono- or di-lower alkylamino, carboxy, lower carbalkoxy, carbamoyl, mono- or di-lower alkylcarbamoyl, HPh, lower alkanoyl or HPhCO)-lower alkyl ; Ph is 1,2-phenylene which can be substituted by at most two members selected from the group consisting of lower alkyl, lower alkoxy, lower alkylthio, halogen and trifluoromethyl ; C2 H2n is lower alkylene separating both nitrogen atoms by 2 or 3 carbon atoms and R5 is hydrogen, lower alkyl, carboxy, lower carbalkoxy or (hydroxy, amino, mono- or di-lower alkylamino)-lower alkyl ; the lower alkoxycarbonyl, lower or higher alkanoyl, adamantoyl, carbamoyl, mono- or di-lower alkylcarbamoyl derivates, cycloalkyl-carbonyl derivatives containing 3 to 7 ring members, or HPhCO-derivatives ; the 2-N-oxide, 2-lower alkyl or 2-HPh-lower alkyl quaternary ammonium derivatives and salts thereof.