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1.发明授权OPTICALLY ACTIVE CARBAMATES, PROCESS FOR PREPARATION THEREOF AND USE THEREOF AS PHARMACEUTICAL INTERMEDIATES 有权光学活性氨基甲酸酯，方法及其及其作为医药中间体
公开(公告)号：EP1963296B1
公开(公告)日：2012-02-15
申请号：EP06831510.0
申请日：2006-12-08
发明人： MEZEI, Tibor , MOLNÁR, Enikö , TRINKA, Péter , BARTHA, Ferenc , KATONA, Zoltán , VERECZKEYNÉ DONÁTH, Györgyi , NAGY, Kálmán , PONGÓ, László , LUKÁCS, Gyula , PORCS-MAKKAY, Márta , ÉVINGER, Zsuzsanna , SIMIG, Gyula
IPC分类号： C07D295/06 , C07D295/18
CPC分类号： C07D295/073 , C07D295/185
摘要： The present invention is related to l-[(4-chlorophenyl)-phenylmethyl]-4-(2,2,2-trichloroethoxycarbonyl)-piperazine of the Formula (IV) and optically isomers thereof, process for preparation thereof and the use of the compound of the Formula (IV) in the preparation of l-(4-chlorophenyl)-phenylmethyl-piperazine and optical isomers and salts thereof. l-(4-chlorophenyl)-phenylmethyl-piperazine and optical isomers thereof are important intermediates in the preparation of non-sedating antihistamine-type active pharmaceutical ingredients.
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公开(公告)号：EP2001464A2
公开(公告)日：2008-12-17
申请号：EP07733842.4
申请日：2007-03-13
发明人： MEZEI, Tibor , SIMIG, Gyula , MOLNÁR, Enikó , SZABÓ, Miklós , LUKÁCS, Gyula , PORCS-MAKKAY, Márta , SZILÁGYI, Erika , BAKÓ, Tibor
IPC分类号： A61K31/381
CPC分类号： C07D333/20
摘要： The subject of the present invention is the provision of new salts of duloxetine of the Formula (I) with organic acids, process for their preparation and medicinal products containing thereof. The new salts are essetially free from the impurity of the Formula (II) and possess high purity and high stability. The new duloxetine salts are prepared by reacting duloxetine free base dissolved in an organic solvent with an approximately equimolar amount of an organic acid. Particularly advantageous crystalline salts are those formed with fumaric acid, citric acid or (-)-mandelic acid.
摘要翻译： 本发明的主题是提供具有式（I）的度洛西汀与有机酸的新盐，其制备方法以及包含其的药物产品。 新盐基本上不含式（II）的杂质且具有高纯度和高稳定性。 新的度洛西汀盐通过溶解在有机溶剂中的度洛西汀游离碱与大约等摩尔量的有机酸反应来制备。 特别有利的结晶盐是与富马酸，柠檬酸或（ - ） - 扁桃酸形成的那些。
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3.发明公开OPTICALLY ACTIVE CARBAMATES, PROCESS FOR PREPARATION THEREOF AND USE THEREOF AS PHARMACEUTICAL INTERMEDIATES 有权光学活性氨基甲酸酯，方法及其及其作为医药中间体
公开(公告)号：EP1963296A2
公开(公告)日：2008-09-03
申请号：EP06831510.0
申请日：2006-12-08
发明人： MEZEI, Tibor , MOLNÁR, Enikö , TRINKA, Péter , BARTHA, Ferenc , KATONA, Zoltán , VERECZKEYNÉ DONÁTH, Györgyi , NAGY, Kálmán , PONGÓ, László , LUKÁCS, Gyula , PORCS-MAKKAY, Márta , ÉVINGER, Zsuzsanna , SIMIG, Gyula
IPC分类号： C07D295/06 , C07D295/18
CPC分类号： C07D295/073 , C07D295/185
摘要： The present invention is related to l-[(4-chlorophenyl)-phenylmethyl]-4-(2,2,2-trichloroethoxycarbonyl)-piperazine of the Formula (IV) and optically isomers thereof, process for preparation thereof and the use of the compound of the Formula (IV) in the preparation of l-(4-chlorophenyl)-phenylmethyl-piperazine and optical isomers and salts thereof. l-(4-chlorophenyl)-phenylmethyl-piperazine and optical isomers thereof are important intermediates in the preparation of non-sedating antihistamine-type active pharmaceutical ingredients.
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