METHOD FOR PREPARING 2,3,3A,4,5,6-HEXAHYDRO-8-CYCLOHEXYL-1H-PYRAZINO(3,2,1-J,K) CARBAZOLE HYDROCHLORIDE AND ANTIDEPRESSIVE DRUG BASED ON THIS COMPOUND

• Main Authors: GORKIN, VLADIMIR Z, SAVITSKAYA, NINA V, ANDREEVA, NATALIA I, ALTUKHOVA, LJUDMILA B, AKALAEVA, TATYANA V, TUPIKINA, SVETLANA M, KONYAEVA, IRINA P, NYRKOVA, VALENTINA G, VERSTAKOVA, OLGA L, VEREVKINA, IREN V, GLUSHKOV, ROBERT G, GRINEV, ALEXEI N. (DECEASED), GUSKOVA, TATYANA A, ARJUZINA, VERA M, FEDOROVA, IRINA N, SHVEDOV, VASILY I, MASHKOVSKY, MIKHAIL D, EROFEEV, JURY V, ASNINA, VALENTINA V, GRINEVA, GALINA V
• Format: Patent
• Language: English; French
• Published: 18.12.1991
• Edition: 5
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

METHOD FOR PREPARING 2,3,3a,4,5,6-EXAXYDRO-8-CYCLOKEXYL-1H-PYRAZIN0(3,2,1,-j,k)CAR3AZOLE HYDROCHLORIDE AND ANTIDEPRESSIVE DRUG BASED ON THIS COMPOUND A method for preparing 2,3,3a,4,5,6-hexahydro-8- -cyclohexyl-1H-pyrazino(3,2,1-j,k)carbazole hydrochloride of the following formula: which involves alkylation of 6-cyclohexyl-3,4-dihydrocar-bazol-1(2H)-one with .beta. -(N,N-dibenzylamino)ethylchlori-de hydrochloride in a two-phase system: an aromatic hydrocarbon 30-40% aqueous solution of an alka1i in the presence of an interphase-transfer catalyst at a temperature of 85-110.degree.C, followed by hydrogenation of the resulting 6-cyclohexyl-9.beta. -(N,N-dibenzylamino)ethyl-3,4-dihydrocar-bazol-1(2H3-one over a palladilIm catalyst supported on a carrier in a lower aliphatic alcohol at a temperature of 50-70.degree.C under a p:ressure of 1 to 30 atm with a subsequent conversion of the resulting 2,3,3a,4,5,6-hexahydro-8-cyclohexyl-1H-pyrazino(3,2,1-jk)-carbazole into hydrochloride and isolation of the latter. The compound according to the present invention exhibits an antidepressive activity and is an active principle of a pharmaceutical preparation possessing an antidepressant effect.