C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/223, 260/265
C07D 487/06 (2006.01) A61K 31/495 (2006.01)
Patent
CA 2019190
METHOD FOR PREPARING 2,3,3a,4,5,6-EXAXYDRO-8- CYCLOKEXYL-1H-PYRAZIN0(3,2,1,-j,k)CAR3AZOLE HYDRO- CHLORIDE AND ANTIDEPRESSIVE DRUG BASED ON THIS COMPOUND Abstract 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: Image 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 hydro- carbon 30-40% aqueous solution of an alka1i in the presence of an interphase-transfer catalyst at a temperatu- re of 85-110°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°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 hydrochlo- ride and isolation of the latter. The compound according to the present invention exhi- bits an antidepressive activity and is an active principle of a pharmaceutical preparation possessing an antidepres- sant effect.
Akalaeva Tatyana V.
Altukhova Ljudmila B.
Andreeva Natalia I.
Arjuzina Vera M.
Asnina Valentina V.
Swabey Ogilvy Renault
Vsesojuzny Nauchno-Issledovatelsky Khimiko-Farmatsevtichesky Ins
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