Process for the manufacture of piperazinopyrrolobenzodiazepines

Details Process for the manufacture of piperazinopyrrolobenzodiazepines Process for the manufacture of piperazinopyrrolobenzodiazepines

C - Chemistry, Metallurgy

07

D

260/239.4, 260/2

C07D 487/14 (2006.01) C07D 207/333 (2006.01) C07D 207/335 (2006.01) C07D 209/48 (2006.01) C07D 487/04 (2006.01)

Patent

CA 1113934

Abstract of the Disclosure The invention concerns the manufacture of new 1,3,4,14b-tetrahydro-2H,1OH-pyrazino[1,2-alpyrrolo[2,1-c [1,4lbenzodlazeplnes of the formula Image (I) wherein each of R1, R3 and R4 is hydrogen or lower alkyl; R2 is hydrogen, lower or higher alkyl, lower alkenyl, lower alkynyl, or (3 to 7 ring-membered cycloalkyl, hydroxy, carboxy, lower carbalkoxy, carbamoyl, HPh, lower alkanoyl or HPhCO)-lower alkyl; Ph is 1,2-phenylene, unsubstituted or substituted by up to two members selected from lower alkyl, lower alkoxy, halogeno and trifluormethyl; CnH2n is lower alkylene separating both nitrogen atoms by 2 or 3 carbon atoms and R5 is hydrogen, lower alkyl, lower carb- alkoxy or hydroxy-lower alkyl; the lower alkoxycarbonyl, lower or higher alkanoyl, adamantoyl, carbamoyl, or HPhCO- derivatives; the 2-N oxide, 2-lower alkyl or 2-HPh-lower alkyl quaternaries of a compound in which R2 is different from hydrogen; and acid addition salts thereof, which exhibit antidepressant, analgesic and antihistaminic properties.

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