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    PROCESS AND INTERMEDIATE FOR THE PRODUCTION OF A TERTIARY ALCOHOL AS AN INTERMEDIATE IN THE SYNTHESIS OF MONTELUKAST
    22.
    发明申请
    PROCESS AND INTERMEDIATE FOR THE PRODUCTION OF A TERTIARY ALCOHOL AS AN INTERMEDIATE IN THE SYNTHESIS OF MONTELUKAST 审中-公开
    在MONTELUKAST合成中作为中间体生产季铵盐的方法和中间体

    公开(公告)号：WO2009010230A3

    公开(公告)日：2009-04-23

    申请号：PCT/EP2008005637

    申请日：2008-07-10

    Applicant: LONZA AG ,  MCGARRITY JOHN ,  DJOJO FRANCIS

    Inventor： MCGARRITY JOHN ,  DJOJO FRANCIS

    IPC: C07D215/18 ,  C07D405/10

    CPC classification number: C07D405/10 ,  C07D215/18

    Abstract: The tertiary alcohol a-[3-[(1E)-2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-2-(1-hydroxy- 1-methylethyl)benzenepropanol, the (aS)-enantioner of which is an intermediate in the production of montelukast, is produced by reacting the novel lactone of formula (II) with a methylmagnesium halide in an ethereal solvent in the presence of lanthanum trichloride and lithium chloride. The lactone II can be prepared by reacting a corresponding hydroxyester with a Grignard reagent in the absence of a lanthanoid compound or with a strong base.

    Abstract translation: 叔醇a- [3 - [（1E）-2-（7-氯-2-喹啉基）乙烯基]苯基] -2-（1-羟基-1-甲基乙基）苯丙醇，（aS） - 苯胺 是制备孟鲁司特的中间体，是通过在三氯化镧和氯化锂的存在下，在醚溶剂中使式（II）的新型内酯与甲基卤化镁反应制备的。 内酯II可以通过在不存在镧系元素化合物或强碱的情况下使相应的羟基酯与格氏试剂反应来制备。

    PROCESS AND INTERMEDIATE FOR THE PRODUCTION OF A TERTIARY ALCOHOL AS AN INTERMEDIATE IN THE SYNTHESIS OF MONTELUKAST
    24.
    发明申请
    PROCESS AND INTERMEDIATE FOR THE PRODUCTION OF A TERTIARY ALCOHOL AS AN INTERMEDIATE IN THE SYNTHESIS OF MONTELUKAST 审中-公开
    制备第三级醇作为中间体合成蒙脱石的方法和中间体

    公开(公告)号：WO2009010230A2

    公开(公告)日：2009-01-22

    申请号：PCT/EP2008/005637

    申请日：2008-07-10

    Applicant: LONZA LTD ,  McGARRITY, John ,  DJOJO, Francis

    Inventor： McGARRITY, John ,  DJOJO, Francis

    IPC: C07D215/18 ,  C07D405/10

    CPC classification number: C07D405/10 ,  C07D215/18

    Abstract: The tertiary alcohol α-[3-[(1 E )-2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-2-(1-hydroxy- 1-methylethyl)benzenepropanol, the (α S )-enantioner of which is an intermediate in the production of montelukast, is produced by reacting the novel lactone of formula (II) with a methylmagnesium halide in an ethereal solvent in the presence of lanthanum trichloride and lithium chloride. The lactone II can be prepared by reacting a corresponding hydroxyester with a Grignard reagent in the absence of a lanthanoid compound or with a strong base.

    Abstract translation: 叔 - 醇[α-[3 - [（E）-2-（7-氯-2-喹啉基）乙烯基]苯基] -2-（1- 其中（αS） - 烯丙醇是孟鲁司特生产中的中间体，是通过将式（Ⅱ）的新内酯与甲基卤化镁在 在三氯化镧和氯化锂存在下的醚溶剂。 内酯II可以通过使相应的羟基酯与格氏试剂在不存在镧系元素化合物或强碱的情况下反应来制备。

    DEUTERIUM-ENRICHED MONTELUKAST
    26.
    发明申请
    DEUTERIUM-ENRICHED MONTELUKAST 审中-公开
    卓越的MONTELUKAST

    公开(公告)号：WO2008157658A1

    公开(公告)日：2008-12-24

    申请号：PCT/US2008/067432

    申请日：2008-06-19

    Applicant: PROTIA LLC ,  CZARNIK, Anthony

    Inventor： CZARNIK, Anthony

    IPC: A01N43/42 ,  A61K31/47 ,  C07D215/18

    CPC classification number: C07D215/18

    Abstract: The present application describes deuterium-enriched montelukast, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

    Abstract translation: 本申请描述了富含氘的孟鲁司特，其药学上可接受的盐形式，以及使用其的治疗方法。

    PROCESS FOR THE PREPARATION OF SODIUM SALT OF L-(((L(R)-(3-(2-(7-CHLORO-2- QUINOLINYL)-ETHENYL)PHENYL)-3-(2-(L-HYDROXY-L- METHYLETHYL)PHENYL)PROPYL)SULFANYL)METHYL)CYCLOPROPANEACETIC ACID
    27.
    发明申请
    PROCESS FOR THE PREPARATION OF SODIUM SALT OF L-(((L(R)-(3-(2-(7-CHLORO-2- QUINOLINYL)-ETHENYL)PHENYL)-3-(2-(L-HYDROXY-L- METHYLETHYL)PHENYL)PROPYL)SULFANYL)METHYL)CYCLOPROPANEACETIC ACID 审中-公开
    制备L - （（（（（R） - （3-（2-（7-氯-2-喹啉基） - 乙烯基）苯基）-3-（2-（L-羟基-L - 甲基）苯基）丙基）磺酰）甲基）环丙烷酸

    公开(公告)号：WO2008136693A2

    公开(公告)日：2008-11-13

    申请号：PCT/PL2008/000033

    申请日：2008-04-30

    Applicant: ZAKLADY FARMACEUTYCZNE POLPHARMA SA ,  ZYLA, Daniel ,  RYNKIEWICZ, Robert ,  KRZYZANOWSKI, Mariusz ,  RAMZA, Jan

    Inventor： ZYLA, Daniel ,  RYNKIEWICZ, Robert ,  KRZYZANOWSKI, Mariusz ,  RAMZA, Jan

    IPC: C07D215/18

    CPC classification number: C07D215/18

    Abstract: The invention relates to a novel process for the preparation of Sodium salt of 1- (((l(R)-(3-(2-(7-chloro-2-quinolinyl)-ethenyl)phenyl)-3-(2-(l-hydroxy-l- methylethyl)phenyl) propyl)sulfanyl)methyl)cyclopropaneacetic acid wherein the crystalline forms of methanesulfonate and Montelukast are not isolated. Furthermore, the invention relates to a novel process for preparing salt of 1-(((1(R)- (3-(2-(7-chloro-2-quinolinyl)-ethenyl)phenyl)-3-(2-(l-hydroxy-l- methylethyl)phenyl)propyl)sulfanyl)methyl)cyclopropaneacetic acid with tert- butylamine and the method for its purification to achieve pharmaceutical purity.

    Abstract translation: 本发明涉及一种制备1-（（（（（（（R） - （3-（2-（7-氯-2-喹啉基） - 乙烯基）苯基）-3-（2- （1-羟基-1-甲基乙基）苯基）丙基）硫烷基）甲基）环丙烷乙酸，其中不分离甲磺酸盐和孟鲁司特的结晶形式。 此外，本发明涉及制备1 - （（（（1（R） - （3-（2-（7-氯-2-喹啉基） - 乙烯基）苯基）-3-（2-（ 1-羟基-1-甲基乙基）苯基）丙基）硫烷基）甲基）环丙烷乙酸与叔丁胺及其纯化方法来获得药物纯度。

    PROCESS FOR THE PREPARATION OF OPTICALLY ACTIVE ETHENYLPHENYL ALCOHOLS
    28.
    发明申请
    PROCESS FOR THE PREPARATION OF OPTICALLY ACTIVE ETHENYLPHENYL ALCOHOLS 审中-公开
    制备光学活性亚乙基醇的方法

    公开(公告)号：WO2008131932A1

    公开(公告)日：2008-11-06

    申请号：PCT/EP2008/003374

    申请日：2008-04-25

    Applicant: LONZA AG ,  MCGARRITY, John ,  BAPPERT, Erhard ,  BELSER, Thomas

    Inventor： MCGARRITY, John ,  BAPPERT, Erhard ,  BELSER, Thomas

    IPC: C07D215/18

    CPC classification number: C07D215/18

    Abstract: Optically active ethenylphenyl-alcohols of formula (I) or its mirror image, wherein R 1 is unsubstituted or substituted heteroaryl and R 2 is phenyl or substituted aryl, are prepared by asymmetric hydrogenation of the corresponding ketones applying hydrogen gas in the presence of specific platinum metal complex catalysts.

    Abstract translation: 式（I）的光学活性乙烯基苯基醇或其镜像，其中R 1是未取代或取代的杂芳基和R 2是苯基或取代的芳基，其通过不对称 在特定的铂金属络合物催化剂的存在下氢化相应的使用氢气的酮。

    A METHOD FOR THE PREPARATION OF MONTELUKAST
    29.
    发明申请
    A METHOD FOR THE PREPARATION OF MONTELUKAST 审中-公开
    一种制备MONTELUKAST的方法

    公开(公告)号：WO2008083635B1

    公开(公告)日：2008-10-09

    申请号：PCT/CZ2008000002

    申请日：2008-01-08

    Applicant: ZENTIVA AS ,  HALAMA ALES ,  JIRMAN JOSEF

    Inventor： HALAMA ALES ,  JIRMAN JOSEF

    IPC: C07D215/18 ,  C07D323/00

    CPC classification number: C07D215/18 ,  C07D323/00

    Abstract: A method of preparation of Montelukast of formula (I) by reaction of the compound of formula (III) and a compound of formula (IX), characterized in that the reaction is carried out in the presence of a base, an inert solvent and a component increasing selectivity of the process, especially of a polyether of general formula (XIII), wherein R stands for hydrogen or an alkyl and the value of n varies from 1 to 40, polyethyleneglycol of general formula (XIV), wherein n=l to 40 or a crown-ether of formulae (XV), (XVI) or (XVII).

    Abstract translation: 通过式（III）化合物与式（IX）化合物的反应制备式（I）的孟鲁司他的方法，其特征在于反应在碱，惰性溶剂和 组分增加了该方法的选择性，特别是通式（XIII）的聚醚，其中R代表氢或烷基，n的值在1至40之间，通式（XIV）的聚乙二醇，其中n = 1至 40或式（XV），（XVI）或（XVII）的冠醚。

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