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    Pyroglutamate salt and use of the same in optical resolution of intermediate for synthesis of dextrocetirizine and levocetirizine
    1.
    发明专利
    Pyroglutamate salt and use of the same in optical resolution of intermediate for synthesis of dextrocetirizine and levocetirizine 审中-公开
    吡喃葡萄糖盐及其在中间体光合作用中的用途，用于合成去氧胆酸酯酶和左旋胆碱酯酶

    公开(公告)号：JP2013032380A

    公开(公告)日：2013-02-14

    申请号：JP2012226914

    申请日：2012-10-12

    Applicant: Ucb Farchim Sa ,  ユセベ ファルシム ソシエテ アノニム

    Inventor： PALACIO MAGALI ,  ATES CELAL

    IPC: C07D295/08 ,  C07B57/00 ,  C07D207/28

    CPC classification number: C07D295/088 ,  C07D207/28

    Abstract: PROBLEM TO BE SOLVED: To provide a simpler preparation method for an enantiomerically and essentially pure compound like levocetirizine or the like by using a novel and enantiomerically and essentially pure intermediate.SOLUTION: There is provided a (S)-2-[4-(4-chlorobenzhydryl)piperazine-1-yl]-ethoxyacetamide-(S)-pyrrolidone-5-carboxylic acid salt, (R)-2-[4-(4-chlorobenzhydryl)piperazine-1-yl]-ethoxyacetamide-(S)-pyrrolidone-5-carboxylic acid salt, (S)-2-[4-(4-chlorobenzhydryl)piperazine-1-yl]-ethoxyacetamide-(R)-pyrrolidone-5-carboxylic acid salt, or (R)-2-[4-(4-chlorobenzhydryl)piperazine-1-yl]-ethoxyacetamide-(R)-pyrrolidone-5-carboxylic acid salt. There is also provided the preparation method for (S)-2-[4-(4-chlorobenzhydryl)piperazine-1-yl]-ethoxyacetamide (I) and (R)-2-[4-(4-chlorobenzhydryl)piperazine-1-yl]-ethoxyacetamide (II) by chemical resolution of a mixture.

    Abstract translation: 要解决的问题：通过使用新型和对映体和基本上纯的中间体，为对映异构体和基本上纯的化合物如左西替利嗪等提供更简单的制备方法。 提供了（S）-2- [4-（4-氯二苯甲基）哌嗪-1-基] - 乙氧基乙酰胺 - （S） - 吡咯烷酮-5-羧酸盐，（R）-2- [（4-氯二苯甲基）哌嗪-1-基] - 乙氧基乙酰胺 - （S） - 吡咯烷酮-5-羧酸盐，（S）-2- [4-（4-氯二苯甲基）哌嗪-1-基] 乙氧基乙酰胺 - （R） - 吡咯烷酮-5-羧酸盐或（R）-2- [4-（4-氯二苯甲基）哌嗪-1-基] - 乙氧基乙酰胺 - （R） - 吡咯烷酮-5-羧酸盐。 还提供了（S）-2- [4-（4-氯二苯甲基）哌嗪-1-基] - 乙氧基乙酰胺（I）和（R）-2- [4-（4-氯二苯甲基）哌嗪-1-基] 吡啶-1-基] - 乙氧基乙酰胺（II）。 版权所有（C）2013，JPO＆INPIT

    Pyroglutamate salts and their use in the optical resolution of intermediates for the synthesis of dextrocetirizine and levocetirizine
    3.
    发明专利
    Pyroglutamate salts and their use in the optical resolution of intermediates for the synthesis of dextrocetirizine and levocetirizine 未知

    公开(公告)号：AU2006222298B2

    公开(公告)日：2011-02-24

    申请号：AU2006222298

    申请日：2006-02-23

    Applicant: UCB FARCHIM SA

    Inventor： PALACIO MAGALI ,  ATES CELAL

    IPC: C07D295/088 ,  C07D207/28

    Abstract: The present invention relates to (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide-(S)-pyrrolidone-5-carboxylic acid salt; (R)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide-(S)-pyrrolidone-5-carboxylic acid salt; (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide-(R)-pyrrolidone-5-carboxylicacid salt; or (R)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxycetamide-(R)-pyrrolidone-5-carboxylic salt. The present invention relates also to a process for preparing (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide (I) and (R)-2-[4-(4-chlorobenzhydryl) piperazin-1-yl]-ethoxyacetamide (II) by chemical resolution of a mixture. These compounds are respectively intermediates for the synthesis of dextrocetirizine and levocetirizine.

    4.
    发明专利
    未知

    公开(公告)号：AT433444T

    公开(公告)日：2009-06-15

    申请号：AT06707220

    申请日：2006-02-23

    Applicant: UCB FARCHIM SA

    Inventor： PALACIO MAGALI ,  ATES CELAL

    IPC: C07D295/088 ,  C07D207/28

    Abstract: The present invention relates to (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide-(S)-pyrrolidone-5-carboxylic acid salt; (R)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide-(S)-pyrrolidone-5-carboxylic acid salt; (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide-(R)-pyrrolidone-5-carboxylicacid salt; or (R)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxycetamide-(R)-pyrrolidone-5-carboxylic salt. The present invention relates also to a process for preparing (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide (I) and (R)-2-[4-(4-chlorobenzhydryl) piperazin-1-yl]-ethoxyacetamide (II) by chemical resolution of a mixture. These compounds are respectively intermediates for the synthesis of dextrocetirizine and levocetirizine.

    ПИРОГЛЮТАМАТЫ И ИХ ПРИМЕНЕНИЕ ДЛЯ РАЗДЕЛЕНИЯ ОПТИЧЕСКИХ ИЗОМЕРОВ ПРОМЕЖУТОЧНЫХ ПРОДУКТОВ СИНТЕЗА ДЕКСТРОЦЕТИРИЗИНА И ЛЕВОЦЕТИРИЗИНА
    5.
    发明专利
    ПИРОГЛЮТАМАТЫ И ИХ ПРИМЕНЕНИЕ ДЛЯ РАЗДЕЛЕНИЯ ОПТИЧЕСКИХ ИЗОМЕРОВ ПРОМЕЖУТОЧНЫХ ПРОДУКТОВ СИНТЕЗА ДЕКСТРОЦЕТИРИЗИНА И ЛЕВОЦЕТИРИЗИНА 未知

    公开(公告)号：EA012575B1

    公开(公告)日：2009-10-30

    申请号：EA200701818

    申请日：2006-02-23

    Applicant: UCB FARCHIM SA

    Inventor： PALACIO MAGALI ,  ATES CELAL

    IPC: C07D295/088 ,  C07D207/28

    Abstract: Визобретенииописанысоль (S)-2-[4-(4-хлорбензгидрил)пиперазин-1-ил]этоксиацетамидас (S)-пирролидон-5-карбоновойкислотой; соль (R)-2-[4-(4-хлорбензгидрил)пиперазин-1-ил]этоксиацетамидас (S)-пирролидон-5-карбоновойкислотой; соль (S)-2-[4-(4-хлорбензгидрил)пиперазин-1-ил]этоксиацетамидас (R)-пирролидон-5-карбоновойкислотойи соль (R)-2-[4-(4-хлорбензгидрил)пиперазин-1-ил]этоксиацетамидас (R)-пирролидон-5-карбоновойкислотой. Визобретениитакжеописанспособполучения (S)-2-[4-(4-хлорбензгидрил)пиперазин-1-ил]этоксиацетамида (I) и (R)-2-[4-(4-хлорбензгидрил)пиперазин-1-ил]этоксиацетамида (II) путемхимическогоразделениясмеси. Этисоединенияявляютсяпромежуточнымипродуктамидлясинтезадекстроцетиризинаи левоцетиризинасоответственно.

    6.
    发明专利
    未知

    公开(公告)号：DE602006007219D1

    公开(公告)日：2009-07-23

    申请号：DE602006007219

    申请日：2006-02-23

    Applicant: UCB FARCHIM SA

    Inventor： PALACIO MAGALI ,  ATES CELAL

    IPC: C07D295/088 ,  C07D207/28

    Abstract: The present invention relates to (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide-(S)-pyrrolidone-5-carboxylic acid salt; (R)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide-(S)-pyrrolidone-5-carboxylic acid salt; (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide-(R)-pyrrolidone-5-carboxylicacid salt; or (R)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxycetamide-(R)-pyrrolidone-5-carboxylic salt. The present invention relates also to a process for preparing (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide (I) and (R)-2-[4-(4-chlorobenzhydryl) piperazin-1-yl]-ethoxyacetamide (II) by chemical resolution of a mixture. These compounds are respectively intermediates for the synthesis of dextrocetirizine and levocetirizine.

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