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    Process for the manufacture of epoxy triazole derivatives
    1.
    发明授权
    Process for the manufacture of epoxy triazole derivatives 有权
    制备环氧三唑衍生物的方法

    公开(公告)号：US08076494B2

    公开(公告)日：2011-12-13

    申请号：US12872599

    申请日：2010-08-31

    Applicant: Marc Muller ,  Lin Xu

    Inventor： Marc Muller ,  Lin Xu

    IPC: C07D309/12 ,  C07D319/06 ,  C07C49/225 ,  C07C49/233 ,  C07F7/18

    CPC classification number: C07D309/12 ,  Y02P20/55

    Abstract: Disclosed is a process for the manufacture of a compound of formula (I) wherein Hal represents fluoro or chloro, and R1 and R2 represent, independently from one another, hydrogen or Hal; in which process a compound of formula (II) is converted to a corresponding alkyl, fluoroalkyl or aryl sulfonic acid ester, which is then reacted with an alkali metal nitrite in the presence of a suitable crown ether in a polar non-nucleophilic solvent at a temperature of −10 to 50° C. to give the compound of formula (I).

    Abstract translation: 公开了制备式（I）化合物的方法，其中Hal表示氟或氯，并且R 1和R 2彼此独立地表示氢或Hal; 在该方法中将式（II）化合物转化为相应的烷基，氟烷基或芳基磺酸酯，然后在极性非亲核溶剂中，在合适的冠醚存在下，与碱金属亚硝酸盐反应， 温度为-10〜50℃，得到式（I）的化合物。

    Process for the manufacture of bridged monobactam intermediates
    2.
    发明申请
    Process for the manufacture of bridged monobactam intermediates 失效
    桥联单体中间体的制备方法

    公开(公告)号：US20110178291A1

    公开(公告)日：2011-07-21

    申请号：US12676580

    申请日：2008-09-15

    Applicant: Marc Muller ,  Xiaoping Wu ,  Lin Xu

    Inventor： Marc Muller ,  Xiaoping Wu ,  Lin Xu

    IPC: C07D205/00 ,  C07C269/00

    CPC classification number: C07C271/54 ,  C07C271/22 ,  C07D487/04

    Abstract: A process for manufacturing a compound of Formula (I) which has cis-conformation and wherein R1 represents a 1-phenyl-C1-C4alkyl or 1-naphthyl-C1-C4alkyl group, wherein the phenyl or naphthyl moiety of R1 is unsubstituted or substituted with one or more C1-C4alkoxy groups and the carbon atoms in 2-, 3-, and/or 4-position of the alkyl part of R1 are, independently of the phenyl or naphthyl moiety of R1 and independently of one another, unsubstituted or substituted with C1-C4alkoxy and/or silyloxy or, preferably, are unsubstituted or substituted with one C1-C4alkoxy group and/or silyloxy group per carbon atom, and R2 represents a C1-C6alkyl group or an unsubstituted or substituted benzyl group, in which process a compound of Formula (II) wherein R3 represents a C1-C6alkyl group or an unsubstituted or substituted benzyl group, and R1 and R2 have the same meaning as in formula (I); is treated with a base at a temperature of 0° C. or less in a liquid aprotic solvent for a time period sufficient to obtain the compound of formula (I).

    Abstract translation: 制备具有顺式构型的式（I）化合物的方法，其中R 1表示1-苯基-C 1 -C 4烷基或1-萘基-C 1 -C 4烷基，其中R 1的苯基或萘基部分是未取代或取代的 与一个或多个C 1 -C 4烷氧基和R 1的烷基部分的2-，3-和/或4-位上的碳原子独立地为R 1的苯基或萘基部分且彼此独立地是未取代的或未取代的 被C1-C4烷氧基和/或甲硅烷氧基取代，或优选未被取代或被每个碳原子一个C1-C4烷氧基和/或甲硅烷氧基取代，R2代表C1-C6烷基或未取代或取代的苄基，其中 处理其中R 3表示C 1 -C 6烷基或未取代或取代的苄基的式（II）化合物，并且R 1和R 2具有与式（I）中相同的含义。 在液体非质子溶剂中在0℃或更低的温度下用碱处理足以获得式（I）化合物的时间段。

    Process for the manufacture of epoxy triazole derivatives
    3.
    发明申请
    Process for the manufacture of epoxy triazole derivatives 有权

    公开(公告)号：US20110021794A1

    公开(公告)日：2011-01-27

    申请号：US12872599

    申请日：2010-08-31

    Applicant: Marc Muller ,  Lin Xu

    Inventor： Marc Muller ,  Lin Xu

    IPC: C07D309/32 ,  C07C45/68

    CPC classification number: C07D309/12 ,  Y02P20/55

    Abstract: Disclosed is a process for the manufacture of a compound of formula (I) wherein Hal represents fluoro or chloro, and R1 and R2 represent, independently from one another, hydrogen or Hal; in which process a compound of formula (II) is converted to a corresponding alkyl, fluoroalkyl or aryl sulfonic acid ester, which is then reacted with an alkali metal nitrite in the presence of a suitable crown ether in a polar non-nucleophilic solvent at a temperature of −10 to 50° C. to give the compound of formula (I).

    Process for the manufacture of epoxybutanol intermediates
    4.
    发明授权
    Process for the manufacture of epoxybutanol intermediates 有权
    制备环氧丁醇中间体的方法

    公开(公告)号：US07816537B2

    公开(公告)日：2010-10-19

    申请号：US12085617

    申请日：2006-11-29

    Applicant: Marc Muller ,  Lin Xu

    Inventor： Marc Muller ,  Lin Xu

    IPC: C07D301/32 ,  C07D303/14 ,  C07D249/08 ,  C07D277/24

    CPC classification number: C07D309/12 ,  Y02P20/55

    Abstract: Disclosed is a process for the manufacture of a compound of formula (I) wherein Hal represents fluoro or chloro, and R1 and R2 represent, independently from one another, hydrogen or Hal; in which process a compound of formula (II) is converted to a corresponding alkyl, fluoroalkyl or aryl sulfonic acid ester, which is then reacted with an alkali metal nitrite in the presence of a suitable crown ether in a polar non-nucleophilic solvent at a temperature of −10 to 50° C. to give the compound of formula (I).

    Abstract translation: 公开了制备式（I）化合物的方法，其中Hal表示氟或氯，并且R 1和R 2彼此独立地表示氢或Hal; 在该方法中将式（II）化合物转化为相应的烷基，氟烷基或芳基磺酸酯，然后在极性非亲核溶剂中，在合适的冠醚存在下，与碱金属亚硝酸盐反应， 温度为-10〜50℃，得到式（I）的化合物。

    Bridged monobactam intermediates
    5.
    发明授权
    Bridged monobactam intermediates 有权
    桥连单体中间体

    公开(公告)号：US08877961B2

    公开(公告)日：2014-11-04

    申请号：US13871338

    申请日：2013-04-26

    Applicant: Marc Muller ,  Xiaoping Wu ,  Lin Xu

    Inventor： Marc Muller ,  Xiaoping Wu ,  Lin Xu

    IPC: C07C67/36 ,  C07D487/04 ,  C07C271/22 ,  C07C271/54

    CPC classification number: C07C271/54 ,  C07C271/22 ,  C07D487/04

    Abstract: C1-C6Alkyloxy- or benzyloxy-carbonyl esters of -{3-[(E)-(1-phenyl or naphthyl C1-C4alkyl)-imino]-propyl}-amino)-acetic acid, which are intermediates for producing known bridged monobactam compounds useful in the treatment of bacterial infections.

    Abstract translation: （3 - [（E） - （1-苯基或萘基C 1 -C 4烷基） - 亚氨基] - 丙基} - 氨基） - 乙酸的C1-C6烷氧基 - 或苄氧基 - 羰基酯，它们是制备已知的桥连单体 可用于治疗细菌感染的化合物。

    Process for the manufacture of bridged monobactam intermediates
    7.
    发明授权
    Process for the manufacture of bridged monobactam intermediates 失效
    桥联单体中间体的制备方法

    公开(公告)号：US08450477B2

    公开(公告)日：2013-05-28

    申请号：US12676580

    申请日：2008-09-15

    Applicant: Marc Muller ,  Xiaoping Wu ,  Lin Xu

    Inventor： Marc Muller ,  Xiaoping Wu ,  Lin Xu

    IPC: C07D487/04 ,  C07C271/22 ,  C07C269/04

    CPC classification number: C07C271/54 ,  C07C271/22 ,  C07D487/04

    Abstract: A process for manufacturing a compound of Formula (I) which has cis-conformation and wherein R1 represents a 1-phenyl-C1-C4alkyl or 1-naphthyl-C1-C4alkyl group, wherein the phenyl or naphthyl moiety of R1 is unsubstituted or substituted with one or more C1-C4alkoxy groups and the carbon atoms in 2-, 3-, and/or 4-position of the alkyl part of R1 are, independently of the phenyl or naphthyl moiety of R1 and independently of one another, unsubstituted or substituted with C1-C4alkoxy and/or silyloxy or, preferably, are unsubstituted or substituted with one C1-C4alkoxy group and/or silyloxy group per carbon atom, and R2 represents a C1-C6alkyl group or an unsubstituted or substituted benzyl group, in which process a compound of Formula (II) wherein R3 represents a C1-C6alkyl group or an unsubstituted or substituted benzyl group, and R1 and R2 have the same meaning as in formula (I); is treated with a base at a temperature of 0° C. or less in a liquid aprotic solvent for a time period sufficient to obtain the compound of formula (I).

    Abstract translation: 制备具有顺式构型的式（I）化合物的方法，其中R 1表示1-苯基-C 1 -C 4烷基或1-萘基-C 1 -C 4烷基，其中R 1的苯基或萘基部分是未取代或取代的 与一个或多个C 1 -C 4烷氧基和R 1的烷基部分的2-，3-和/或4-位上的碳原子独立地为R 1的苯基或萘基部分且彼此独立地是未取代的或未取代的 被C1-C4烷氧基和/或甲硅烷氧基取代，或优选未被取代或被每个碳原子一个C 1 -C 4烷氧基和/或甲硅烷氧基取代，并且R 2表示C 1 -C 6烷基或未取代或取代的苄基，其中 处理其中R 3表示C 1 -C 6烷基或未取代或取代的苄基的式（II）化合物，并且R 1和R 2具有与式（I）中相同的含义。 在液体非质子溶剂中在0℃或更低的温度下用碱处理足以获得式（I）化合物的时间段。

    Process for the Manufacture of Epoxybutanol Intermediates
    8.
    发明申请
    Process for the Manufacture of Epoxybutanol Intermediates 有权
    环氧丁醇中间体的制造工艺

    公开(公告)号：US20090299073A1

    公开(公告)日：2009-12-03

    申请号：US12085617

    申请日：2006-11-29

    Applicant: Marc Muller ,  Lin Xu

    Inventor： Marc Muller ,  Lin Xu

    IPC: C07D277/28 ,  C07D249/08 ,  C07D303/04

    CPC classification number: C07D309/12 ,  Y02P20/55

    Abstract: Disclosed is a process for the manufacture of a Compound of formula (I) wherein Hal represents fluoro or chloro, and R1 and R2 represent, independently from one another, hydrogen or Hal; in which process a Compound of formula (II) is converted to a corresponding alkyl, fluoroalkyl or aryl sulfonic acid ester, which is then reacted with an alkali metal nitrite in the presence of a suitable crown ester in a polar non-nucleophilic solvent at a temperature of −10 to 50° C. to give the Compound of formula (I).

    Abstract translation: 公开了制备式（I）的化合物的方法，其中Hal表示氟或氯，R 1和R 2彼此独立地表示氢或卤素; 在该方法中，将式（II）化合物转化为相应的烷基，氟烷基或芳基磺酸酯，然后在极性非亲核溶剂中，在合适的冠酯存在下，与碱金属亚硝酸盐反应， 温度为-10〜50℃，得到式（I）的化合物。

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