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    PROCESS FOR THE PREPARATION OF PIPERAZINE COMPOUNDS AND HYDROCHLORIDE SALTS THEREOF
    1.
    发明公开
    PROCESS FOR THE PREPARATION OF PIPERAZINE COMPOUNDS AND HYDROCHLORIDE SALTS THEREOF 有权
    用于生产哌嗪和其盐酸盐的

    公开(公告)号：EP2358691A1

    公开(公告)日：2011-08-24

    申请号：EP09797146.9

    申请日：2009-12-18

    申请人： Richter Gedeon Nyrt.

    发明人： CZIBULA, Lászl ,  JUHÁSZ, Bálint ,  ÁGAINÉ CSONGOR, Éva ,  SEBÖK, Ferenc ,  GALAMBOS, János ,  N GRÁDI, Katalin

    IPC分类号： C07D295/135

    CPC分类号： C07D295/135

    摘要： The invention relates to a new process for the preparation of compounds of general formula (I) and hydrochloric acid alts and/or hydrates and/or solvates thereof, by dissolving suspending trans 4-[2-[4-(2,3-dichlorophenyl)-piperazine1-il]-cyclohexylamine of formula (III) or a salt or a hydrate or a solvate thereof in an inert solvent in the presence base then adding a carbonic acid derivative of general formula (VI) wherein R is alkyl with C
    1-6 straight or branched chain or C
    1-2 fully halogenated alkyl, Z is -O-R or -X, wherein R is as described above, X is halogen, and reacting the compound of general formula (IV) obtained wherein R is as described above, in situ or, optionally in isolated state with an amine of general formula (V) wherein R
    1 and R
    2 are as described above to obtain the compound of general formula (I) and then optionally forming the hydrochloride salts and/or hydrates and/or solvates thereof.

    PROCESS FOR THE PREPARATION OF TRANS 4-AMINO-CYCLOHEXYL ACETIC ACID ETHYL ESTER HCL
    2.
    发明公开
    PROCESS FOR THE PREPARATION OF TRANS 4-AMINO-CYCLOHEXYL ACETIC ACID ETHYL ESTER HCL 有权
    制备反式4-氨基环己基醋酸乙酯盐酸盐的方法

    公开(公告)号：EP2358661A1

    公开(公告)日：2011-08-24

    申请号：EP09797144.4

    申请日：2009-12-17

    申请人： Richter Gedeon Nyrt.

    发明人： MÁTHÉ, Tibor, Bence ,  HEGEDÚS, László ,  CZIBULA, László ,  JUHÁSZ, Bálint ,  NAGYNÉ BAGDY, Judit ,  MÁRKOS, Dénes

    IPC分类号： C07C227/04 ,  C07C227/16 ,  C07C227/18 ,  C07C229/46

    CPC分类号： C07C229/46 ,  C07C61/08 ,  C07C227/04 ,  C07C227/16 ,  C07C227/18 ,  C07C229/40 ,  C07C2601/14 ,  C07C229/42

    摘要： The invention relates to a process for the preparation of trans 4-amino-cyclohexil ethyl acetate HCl wherein d) hydrogenating 4-nitrophenyl acetic acid in a protic solvent at a temperature between 40-500C in the presence of Pd/C under 0.1-0.6 bar overpressure, and e) further hydrogenating the 4-aminophenyl acetic acid obtained in situ in step a) at a temperature between 50-60 0C under 1-4 bar overpressures, then f) heating to reflux the 4-aminocyclohexil acetic acid obtained in step b) for 1-3 hours in hydrochloric ethanol, and if desired after removing the solvent acetonitrile was added to the residue obtained and distilled off.

    摘要翻译： 本发明涉及制备反式4-氨基 - 环己基乙酸乙酯HCl的方法，其中d）在质子溶剂中，在Pd / C存在下，在40-60℃的温度下，在0.1-0.6的温度下氢化4-硝基苯基乙酸 e）将在步骤a）中原位获得的4-氨基苯基乙酸在50-60℃的温度和1-4巴的超压下进一步氢化，然后f）加热回流在步骤a）中得到的4-氨基环己基乙酸 步骤b）在盐酸乙醇中处理1-3小时，如果需要，除去溶剂后，将乙腈加入到所得残余物中并蒸馏出。

    PROCESS FOR THE PREPARATION OF PIPERAZINE DERIVATIVES
    7.
    发明公开
    PROCESS FOR THE PREPARATION OF PIPERAZINE DERIVATIVES 有权
    用于生产哌嗪衍生物

    公开(公告)号：EP2367807A1

    公开(公告)日：2011-09-28

    申请号：EP09797147.7

    申请日：2009-12-18

    申请人： Richter Gedeon Nyrt.

    发明人： ÁGAINÉ CSONGOR, Éva ,  CZIBULE, László ,  SEBÖK, Ferenc ,  JUHÁSZ, Bálint ,  GALAMBOS, János ,  NÓGRÁDI, Katalin

    IPC分类号： C07D295/135

    CPC分类号： C07D295/135

    摘要： The invention relates to a process for the preparation of the trans
    N-{ 4-{2-[4-(2,3- dichlorophenyl)-piperazine-1-yl]-ethyl}-cyclohexyl}-carbamide derivatives of formula (I) by reacting the compound of formula (III) with a carbamoylchloride of formula (II) which comprises carrying out the reaction in a mixture of a solvent and concentrated aqueous solution of an alkali hydroxide at a temperature between 40-100 °C in the presence of a phase transfer catalyst, separating the phases and washing the organic layer then removing the solvent and drying the compound of formula (I) obtained until its weight is constant.