公开(公告)号：EP0457908A1

公开(公告)日：1991-11-27

申请号：EP90905365.4

申请日：1989-11-27

申请人： VSESOJUZNY NAUCHNO-ISSLEDOVATELSKY KHIMIKO-FARMATSEVTICHESKY INST. IMENI SERGO ORDZHONIKIDZE (VNIKHFI)

发明人： SHVEDOV, Vasily Ivanovich ,  MASHKOVSKY, Mikhail Davydovich ,  SAVITSKAYA, Nina Viktorovna ,  ANDREEVA, Natalia Ivanovna ,  FEDOROVA, Irina Nikolaevna ,  GUSKOVA, Tatyana Anatolievna ,  TUPIKINA, Svetlana Mikhailovna ,  VERSTAKOVA, Olga Lvovna ,  NYRKOVA, Valentina Georgievna ,  KONYAEVA, Irina Pavlovna ,  ALTUKHOVA, Ljudmila Benediktovna ,  AKALAEVA, Tatyana Vasilievna ,  ASNINA, Valentina Vasilievna ,  GORKIN, Vladimir Zinovievich ,  VEREVKINA, Iren Vladimirovna ,  GLUSHKOV, Robert Georgievich ,  ARJUZINA, Vera Mikhailovna ,  EROFEEV, Jury Vladimirovich ,  GRINEV, Alexei Nikolaevich

IPC分类号： C07D487/04 ,  A61K31/495

CPC分类号： C07D487/06

摘要： Hydrochloride 2,3,3a,4,5,6-hexahydro-8-cyclohexyl-1H-pyrazino (3,2,1-j,k)carbazol has formula (I). A method of obtaining the claimed composition consists in that 6-cyclohexyl-3,4-dihydrocarbazol-1(2H) is alkylated by hydrochloride β-(N,N-dibenzylamino) ethylchloride in a two-phase system: an aromatic hydrocarbon-34-40 %-aqueous solution of alkali in the presence of an interphase transfer catalyst at a temperature of 85-110 °C with subsequent hydrogenation of the resulting 6-cyclohexyl-9β-(N,N-dibenzylamino) ethyl-3,4-dihydrocarbazol-1(2H) over palladium catalyst on a carrier in the medium of a higher aliphatic alcohol at a temperature of 50-70 °C and under a pressure of 1 to 30 atm with subsequent transfer of the obtained 2,3,3a,4,5,6-hexahydro-8-cyclohexyl-1H-pyrazino (3,2,1-j,k)carbazol into hydrochloride and extraction of the latter. The claimed composition has an antidepressive action and is an active substance of a pharmaceutical preparation with antidepressive action.

摘要翻译： 盐酸盐4,5,6-2,3,3a六氢-8-环己基-1H-吡嗪并（3,2,1-J，K）咔唑具有式（I）。 获得的要求的组合物besteht，DASS的方法6-环己基-3,4-二氢咔唑-1（2H）是由盐酸盐的β烷基化 - （N，N-二苄基氨基）乙基氯在两相体系：芳族烃-34 （N，N-二苄基氨基）乙基-3,4- - 在相间转移催化剂的存在下，在85-110℃下与所得的6-环己基9的β随后氢化的温度的碱-40％的水溶液 -dihydrocarbazol-1（2H）超过在50-70℃的温度和1至30个大气压与所获得的甲基-2,3,3a的后续传送的压力下，在更高的脂族醇的介质中的载体上的钯催化剂 ，4,5,6-六氢-8-环己基-1H-吡嗪并（3,2,1-J，K）咔唑为盐酸和后者的提取。 所要求保护的组合物具有抗抑郁作用，并且与抗抑郁作用的药物制剂的活性物质。