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    PIPERAZINE SALT AND A PROCESS FOR THE PREPARATION THEREOF
    2.
    发明公开
    PIPERAZINE SALT AND A PROCESS FOR THE PREPARATION THEREOF 有权
    哌嗪和方法及其

    公开(公告)号：EP2358690A1

    公开(公告)日：2011-08-24

    申请号：EP09797145.1

    申请日：2009-12-17

    申请人： Richter Gedeon Nyrt.

    发明人： CZIBULA, Lászl ,  ÁGAINÉ CSONGOR, Éva ,  NOGRADI, Katalin ,  JUHASZ, Bálint ,  SEBOK, Ferenc ,  GALAMBOS, János ,  VAGO, István

    IPC分类号： C07D295/135

    CPC分类号： C07D295/135

    摘要： The invention relates to novel trans N-{4-{2-[4-(2,3-dichlorophenyl)-piperazine-l-il]-ethyl}- cyclohexylamine dihydrochloride monohydrate and a process for the preparation of the trans N- {4- {2-[4-(2,3-dichlorophenyl)-piperazine-l -il]-ethyl}-cyclohexylamine dihydrochloride monohydrate, said process comprising the steps a) reacting trans 2-{l-[4-(N-tert-butoxycarbonyl)amino]- cyclohexyl} -acetic acid ester with sodium borohydride and aluminium trichloride to give trans 2-{l-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethanol; b) reacting trans 2-{l-[4-(N-tert-butoxycarbonyl)-amino]cyclohexyl}-ethanol obtained with methanesulfonic acid chloride in the presence of an acid binding agent to give trans 2-{l-[4- (N-tert-butoxycarbonyl)-amino] -cyclohexyl} -ethyl methanesulfonate; c) reacting trans 2-{l-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethyl methanesulfonate obtained with 2,3-dichlorophenyl-piperazine in the presence of an acid binding agent to give trans 2-{l-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-carbamic acid tert-butylester; d) heating trans 2-{l-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-carbamic acid tert- butylester obtained to a temperature between 40-100°C in a mixture of aqueous hydrochloric acid/methanol to give trans N-{4-{2-[4-(2,3-dichlorophenyl)piperazine-l-il]-ethyl}- cyclohexylamine dihydrochloride monohydrate.