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    Process for the preparation of azithromycin monohydrate isopropanol clathrate
    1.
    发明申请
    Process for the preparation of azithromycin monohydrate isopropanol clathrate 失效
    制备阿奇霉素一水合异丙醇包合物的方法

    公开(公告)号：US20060019908A1

    公开(公告)日：2006-01-26

    申请号：US11166250

    申请日：2005-06-27

    申请人： Dhiren Mistry ,  Mahadeo Thorat ,  Kamlesh Soni ,  Vinod Kansal

    发明人： Dhiren Mistry ,  Mahadeo Thorat ,  Kamlesh Soni ,  Vinod Kansal

    IPC分类号： A61K31/7052 ,  C07H17/08

    CPC分类号： C07H17/08

    摘要： The present invention relates to an improved, cost effective and easy process for the preparation of azithromycin monohydrate isopropanol clathrate. The process provides a one-step method of preparing azithromycin monohydrate isopropanol clathrate directly from 9-deoxo-9a-aza-9a-homoerythromycin A. The process comprises at least partial dissolution and/or suspension of 9-deoxo-9a-aza-9a homoerythromycin A in isopropanol to form a mixture, adding methylating solution to the said mixture, refluxing or heating said mixture to form a reaction mixture, adding alkaline solution to the reaction mixture to adjust pH from about 10 to about 11 and isolating pure azithromycin monohydrate isopropanol clathrate. The process helps in reducing the total time of preparation, total utility cost for the production and also helps to avoid handling loss.

    摘要翻译： 本发明涉及一种用于制备阿奇霉素一水合物异丙醇包合物的改进的，成本有效和容易的方法。 该方法提供了直接从9-脱氧-9a-氮杂-9a-高红霉素A制备阿奇霉素一水合物异丙醇包合物的一步法。该方法至少部分溶解和/或悬浮9-脱氧-9a-氮杂-9a 同型红霉素A在异丙醇中形成混合物，向所述混合物中加入甲基化溶液，回流或加热所述混合物以形成反应混合物，向反应混合物中加入碱性溶液以将pH调节至约10至约11，并分离纯的阿奇霉素一水合异丙醇 包合物 该过程有助于缩短制备的总时间，生产的总用电成本，并有助于避免处理损失。

    Process for the preparation of biologically active tetrahydrobenzthiazole derivative
    2.
    发明申请
    Process for the preparation of biologically active tetrahydrobenzthiazole derivative 审中-公开

    公开(公告)号：US20070123573A1

    公开(公告)日：2007-05-31

    申请号：US10588564

    申请日：2005-04-25

    申请人： Dhiren Mistry ,  Kamlesh Soni ,  Sanjay Vasoya ,  Vinod Kansal

    发明人： Dhiren Mistry ,  Kamlesh Soni ,  Sanjay Vasoya ,  Vinod Kansal

    IPC分类号： A61K31/428 ,  C07D277/82

    CPC分类号： C07D277/82

    摘要： Improved process for the preparation of the intermediate compound of formula II for formation of biological active tetrahydrobenzothiazole compound of formula (I) as well as the biological active tetrahydrobenzothiazole compound of formula (I) and/or its pharmaceutically acceptable salts or solvates. The process comprises reacting 4-amino cyclohexanol of formula (III) or its acid addition salts with phthalic anhydride in presence of acid catalyst and their salts, in polar aprotic solvent or its mixture with organic solvent, capable of removing water azeotropically to give 4-(phthalimido)-cyclohexanol of formula (IV); oxidizing 4-(phthalimido)-cyclohexanol of formula (IV) to give 4-(phthalimido)-cyclohexanone of formula (V); brominating 4-(phthalimido)-cyclohexanone of formula (V) with brominating agent in organic solvent in presence of Lewis acid catalyst to prepare 2-bromo-4-(phthalimido)-cyclohexanone of formula (VI); treating 2-bromo-4-(phthalimido)-cyclohexanone of formula (VI) with thiourea in organic solvent in presence of base to give 2-amino-6-phthalimido-4,5,6,7-tetrahydro benzothiazol of formula (VII); reacting compound of formula (VII) with hydrazine hydrate and base in polar solvent to give racemic 2,6-diamino-4,5,6,7-tetrahydro-1,3-benzothiazole of formula (VIII); resolving racemic 2,6-diamino-4,5,6,7-tetrahydro-1,3-benzothiazole of formula (VIII) to prepare (6S)-2,6-diamino-4,5,6,7-tetrahydro-1,3-benzothiazole of formula (II). To form the compound of Formula I and if desired its salts/solvates the above process is carried out with further steps of coupling (6S)-2,6-dimino-4,5,6,7-tetrahydro-1,3-benzothiazole of formula (II) with propionaldehyde in presence of mineral acid in polar organic solvent and reducing agent to prepare (S)-(−)-2-Amino-6-(n-propylamino)-4,5,6,7-tetrahydrobenzothiazole of formula (I);and if desired converting (S)-(−)-2-Amino-6-(propylamino)-4,5,6,7-tetrahydrobenzothiazole to its pharmaceutically acceptable salts or solvates.

    Processes for the preparation of (3R,4S)-4-((4-benzyloxy)phenyl)-1-(4-fluorophenyl)-3-((S)-3-(4-fluorophenyl)-3-hydroxypropyl)-2-azetidinone, an intermediate for the synthesis of ezetimibe
    9.
    发明申请
    Processes for the preparation of (3R,4S)-4-((4-benzyloxy)phenyl)-1-(4-fluorophenyl)-3-((S)-3-(4-fluorophenyl)-3-hydroxypropyl)-2-azetidinone, an intermediate for the synthesis of ezetimibe 审中-公开
    制备（3R，4S）-4 - （（4-苄氧基）苯基）-1-（4-氟苯基）-3 - （（S）-3-（4-氟苯基）-3-羟丙基） - 2-氮杂环丁酮，合成依泽替米贝的中间体

    公开(公告)号：US20070259845A1

    公开(公告)日：2007-11-08

    申请号：US11517704

    申请日：2006-09-08

    申请人： Vinod Kansal ,  Suhail Ahmad ,  Bhupendra Tyagi ,  Nitin Gupta ,  Nurit Perlman

    发明人： Vinod Kansal ,  Suhail Ahmad ,  Bhupendra Tyagi ,  Nitin Gupta ,  Nurit Perlman

    IPC分类号： A61K31/397 ,  A61P9/12 ,  C07D205/00

    CPC分类号： C07D205/08 ,  Y02P20/55

    摘要： The invention encompasses (3R,4S)-4-((4-benzyloxy)phenyl)-1-(4-fluorophenyl)-3-(3-(4-fluorophenyl)-3-oxopropyl)-2-azetidinone (Compound 2a) having an enantiomeric purity of at least about 97.5%. The invention also encompasses Compound 2a having a chemical purity of at least about 97%. The invention further encompasses processes for preparing Compound 2a from Compound 1 having the following formula: The invention also encompasses processes for preparing a compound having the following formula: from a compound having the following formula: wherein R is selected from the group consisting of: H or a hydroxyl protecting group. The invention also encompasses processes for preparing Compound 2a, preferably to form Compound 2a-Form 01. Also included are processes for preparing ezetimibe from Compound 2a-Form 01 or Compound 2a prepared according to the invention, compositions containing such ezetimibe, and methods for reducing cholesterol using such compositions.

    摘要翻译： 本发明包括（3R，4S）-4 - （（4-苄氧基）苯基）-1-（4-氟苯基）-3-（3-（4-氟苯基）-3-氧代丙基）-2-氮杂环丁酮（化合物2a ）具有至少约97.5％的对映体纯度。 本发明还包括具有至少约97％的化学纯度的化合物2a。 本发明还包括从具有下式的化合物1制备化合物2a的方法：本发明还包括由具有下式的化合物制备具有下式的化合物的方法：其中R选自：H 或羟基保护基。 本发明还包括制备化合物2a，优选形成化合物2a-形式01的方法。还包括用于制备根据本发明制备的化合物2a-形式01或化合物2a的依泽替米贝的方法，含有这种依泽替米贝的组合物，以及还原方法 使用这种组合物的胆固醇。