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    Process for the production of cyclopropane derivatives
    3.
    发明授权
    Process for the production of cyclopropane derivatives 有权
    制备环丙烷衍生物的方法

    公开(公告)号：US08497384B2

    公开(公告)日：2013-07-30

    申请号：US13129213

    申请日：2009-11-12

    申请人： Mehul Thathagar ,  Peter Poechlauer ,  Sascha Braune

    发明人： Mehul Thathagar ,  Peter Poechlauer ,  Sascha Braune

    IPC分类号： C07D333/78

    CPC分类号： C07B37/10 ,  C07D333/78 ,  Y02P20/582

    摘要： A process for the preparation of a cyclopropane derivative of Formula (I), by reacting an olefin of Formula (II), with a carbene of the formula:CR1R2, in a reaction vessel, optionally in the presence of a solvent, wherein, R1 and R2 are each independently hydrogen, C1-C6 alkyl, C2-C6 alkenyl, aryl, heteroaryl, heterocyclyl, carbocyclyl, heterocyclyl, —C(O)R7 or —NR82; R3, R4, R5 and R6 are each independently hydrogen, C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, aryl, aryloxy, heteroaryl, heterocyclyl, carbocyclyl, heterocyclyl, —C(O)R9, —NR102, —SR11, —S(O)R11, or —SO2R11, or R3 and R6 are as defined above and R4 and R5 together form a ring, which ring is carbocyclyl, heterocyclyl, aromatic or heteroaromatic; R7 is hydrogen, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, aryl, aryloxy, heteroaryl or —NR102; R8 is hydrogen, C1-C6 alkyl, C1-C6 alkenyl, aryl, heteroaryl, carbocyclyl or heterocyclyl; R9 is hydrogen, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, aryl, aryloxy or heteroaryl; R10 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, aryl, heteroaryl, carbocyclyl, heterocyclyl or C(O)R12; R11 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, aryl, heteroaryl, carbocyclyl or heterocyclyl; and R12 is hydrogen, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, aryl, or aryloxy, in the presence of copper metal or copper oxide, wherein the process is a continuous process.

    摘要翻译： 一种制备式（I）的环丙烷衍生物的方法，通过使式（II）的烯烃与式CR1R2的卡宾反应在反应容器中，任选地在溶剂存在下，其中R 1 C 1 -C 6烷基，C 2 -C 6烯基，芳基，杂芳基，杂环基，碳环基，杂环基，-C（O）R 7或-NR 82; R3，R4，R5和R6各自独立地为氢，C1-C6烷基，C1-C6烷氧基，C2-C6烯基，芳基，芳氧基，杂芳基，杂环基，碳环基，杂环基，-C（O）R9，-NR102， SR11，-S（O）R11或-SO2R11，或R3和R6如上定义，R4和R5一起形成环，该环是碳环基，杂环基，芳族或杂芳族; R 7是氢，羟基，C 1 -C 6烷基，C 1 -C 6烷氧基，芳基，芳氧基，杂芳基或-NR 102; R 8是氢，C 1 -C 6烷基，C 1 -C 6烯基，芳基，杂芳基，碳环基或杂环基; R9是氢，羟基，C1-C6烷基，C1-C6烷氧基，芳基，芳氧基或杂芳基; R 10是氢，C 1 -C 6烷基，C 2 -C 6烯基，芳基，杂芳基，碳环基，杂环基或C（O）R 12; R11是氢，C1-C6烷基，C2-C6烯基，芳基，杂芳基，碳环基或杂环基; 并且在铜金属或氧化铜的存在下，R 12是氢，羟基，C 1 -C 6烷基，C 1 -C 6烷氧基，芳基或芳氧基，其中该方法是连续方法。

    PROCESS FOR THE PRODUCTION OF CYCLOPROPANE DERIVATIVES
    4.
    发明申请
    PROCESS FOR THE PRODUCTION OF CYCLOPROPANE DERIVATIVES 有权
    生产环丙基衍生物的方法

    公开(公告)号：US20110301359A1

    公开(公告)日：2011-12-08

    申请号：US13129213

    申请日：2009-11-12

    申请人： Mehul Thathagar ,  Peter Poechlauer ,  Sascha Braune

    发明人： Mehul Thathagar ,  Peter Poechlauer ,  Sascha Braune

    IPC分类号： C07D333/78

    CPC分类号： C07B37/10 ,  C07D333/78 ,  Y02P20/582

    摘要： A process for the preparation of a cyclopropane derivative of Formula (I), by reacting an olefin of Formula (II), with a carbene of the formula: CR1R2, in a reaction vessel, optionally in the presence of a solvent, wherein, R1 and R2 are each independently hydrogen, C1-C6 alkyl, C2-C6 alkenyl, aryl, heteroaryl, heterocyclyl, carbocyclyl, heterocyclyl, —C(O)R7 or —NR82; R3, R4, R5 and R6 are each independently hydrogen, C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, aryl, aryloxy, heteroaryl, heterocyclyl, carbocyclyl, heterocyclyl, —C(O)R9, —NR102, —SR11, —S(O)R11, or —SO2R11, or R3 and R6 are as defined above and R4 and R5 together form a ring, which ring is carbocyclyl, heterocyclyl, aromatic or heteroaromatic; R7 is hydrogen, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, aryl, aryloxy, heteroaryl or —NR102; R8 is hydrogen, C1-C6 alkyl, C1-C6 alkenyl, aryl, heteroaryl, carbocyclyl or heterocyclyl; R9 is hydrogen, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, aryl, aryloxy or heteroaryl; R10 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, aryl, heteroaryl, carbocyclyl, heterocyclyl or C(O)R12; R11 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, aryl, heteroaryl, carbocyclyl or heterocyclyl; and R12 is hydrogen, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, aryl, or aryloxy, in the presence of copper metal or copper oxide, wherein the process is a continuous process.

    摘要翻译： 一种制备式（I）的环丙烷衍生物的方法，通过使式（II）的烯烃与式CR1R2的卡宾反应在反应容器中，任选地在溶剂存在下，其中R 1 C 1 -C 6烷基，C 2 -C 6烯基，芳基，杂芳基，杂环基，碳环基，杂环基，-C（O）R 7或-NR 82; R3，R4，R5和R6各自独立地为氢，C1-C6烷基，C1-C6烷氧基，C2-C6烯基，芳基，芳氧基，杂芳基，杂环基，碳环基，杂环基，-C（O）R9，-NR102， SR11，-S（O）R11或-SO2R11，或R3和R6如上定义，R4和R5一起形成环，该环是碳环基，杂环基，芳族或杂芳族; R 7是氢，羟基，C 1 -C 6烷基，C 1 -C 6烷氧基，芳基，芳氧基，杂芳基或-NR 102; R 8是氢，C 1 -C 6烷基，C 1 -C 6烯基，芳基，杂芳基，碳环基或杂环基; R9是氢，羟基，C1-C6烷基，C1-C6烷氧基，芳基，芳氧基或杂芳基; R 10是氢，C 1 -C 6烷基，C 2 -C 6烯基，芳基，杂芳基，碳环基，杂环基或C（O）R 12; R11是氢，C1-C6烷基，C2-C6烯基，芳基，杂芳基，碳环基或杂环基; 并且在铜金属或氧化铜的存在下，R 12是氢，羟基，C 1 -C 6烷基，C 1 -C 6烷氧基，芳基或芳氧基，其中该方法是连续方法。

    Continuous production and reaction of a diazo compound
    5.
    发明授权
    Continuous production and reaction of a diazo compound 有权
    连续生产和重氮化合物的反应

    公开(公告)号：US09249088B2

    公开(公告)日：2016-02-02

    申请号：US13879889

    申请日：2011-11-01

    申请人： Peter Poechlauer ,  Rafael Wilhelmus Elisabeth Ghislain Reintjens ,  Hubertus Johannes Adrianus Dielemans ,  Mehul Thathagar ,  Jeroen Hubertina Gerardus Konings

    发明人： Peter Poechlauer ,  Rafael Wilhelmus Elisabeth Ghislain Reintjens ,  Hubertus Johannes Adrianus Dielemans ,  Mehul Thathagar ,  Jeroen Hubertina Gerardus Konings

    IPC分类号： C07C245/16 ,  C07C67/00 ,  C07C245/14 ,  C07D231/06

    CPC分类号： C07C245/16 ,  C07C67/00 ,  C07C245/14 ,  C07D231/06 ,  C07C69/78

    摘要： A process for producing a reaction product of a diazo compound, which process comprises: a. continuously supplying to a first reactor a precursor of a diazo compound; a water-miscible solvent; a base and water; b. mixing the precursor of a diazo compound; the water-miscible solvent; the base and water to generate a diazo compound; c. continuously removing from the first reactor, through a hydrophobic membrane, into a second reactor the formed diazo compound; d. continuously removing from the first reactor all reaction products that have not passed into the second reactor; e. continuously supplying to the second reactor a substrate in a non-water-miscible solvent; f. mixing the above components to generate a reaction product of a diazo compound; and g. continuously removing from the second reactor the non-water-miscible solvent and the reaction product of the diazo compound, and apparatus suitable for carrying out such a process.

    摘要翻译： 一种制备重氮化合物的反应产物的方法，该方法包括：a。 向第一反应器连续供应重氮化合物的前体; 水溶性溶剂; 基地和水; b。 混合重氮化合物的前体; 水溶性溶剂; 碱和水生成重氮化合物; C。 连续地从第一反应器中通过疏水膜除去形成的重氮化合物的第二反应器; d。 从第一反应器中连续除去未进入第二反应器的所有反应产物; e。 在非水混溶性溶剂中连续向第二反应器供给基材; F。 混合上述组分以产生重氮化合物的反应产物; 和g。 从第二反应器中连续除去非水混溶性溶剂和重氮化合物的反应产物，以及适于进行这种方法的设备。

    CONTINUOUS PRODUCTION AND REACTION OF A DIAZO COMPOUND
    6.
    发明申请
    CONTINUOUS PRODUCTION AND REACTION OF A DIAZO COMPOUND 有权
    连续生产和反应的DIAZO化合物

    公开(公告)号：US20140100360A1

    公开(公告)日：2014-04-10

    申请号：US13879889

    申请日：2011-11-01

    申请人： Peter Poechlauer ,  Rafael Wilhelmus Elisabeth Ghislain Reintjens ,  Hubertus Johannes Adrianus Dielemans ,  Mehul Thathagar ,  Jeroen Hubertina Gerardus Konings

    发明人： Peter Poechlauer ,  Rafael Wilhelmus Elisabeth Ghislain Reintjens ,  Hubertus Johannes Adrianus Dielemans ,  Mehul Thathagar ,  Jeroen Hubertina Gerardus Konings

    IPC分类号： C07C245/16

    CPC分类号： C07C245/16 ,  C07C67/00 ,  C07C245/14 ,  C07D231/06 ,  C07C69/78

    摘要： A process for producing a reaction product of a diazo compound, which process comprises: a. continuously supplying to a first reactor a precursor of a diazo compound; a water-miscible solvent; a base and water; b. mixing the precursor of a diazo compound; the water-miscible solvent; the base and water to generate a diazo compound; c. continuously removing from the first reactor, through a hydrophobic membrane, into a second reactor the formed diazo compound; d. continuously removing from the first reactor all reaction products that have not passed into the second reactor; e. continuously supplying to the second reactor a substrate in a non-water-miscible solvent; f. mixing the above components to generate a reaction product of a diazo compound; and g. continuously removing from the second reactor the non-water-miscible solvent and the reaction product of the diazo compound, and apparatus suitable for carrying out such a process.

    摘要翻译： 一种制备重氮化合物的反应产物的方法，该方法包括：a。 向第一反应器连续供应重氮化合物的前体; 水溶性溶剂; 基地和水; b。 混合重氮化合物的前体; 水溶性溶剂; 碱和水生成重氮化合物; C。 连续地从第一反应器中通过疏水膜除去形成的重氮化合物的第二反应器; d。 从第一反应器中连续除去未进入第二反应器的所有反应产物; e。 在非水混溶性溶剂中连续向第二反应器供给基材; F。 混合上述组分以产生重氮化合物的反应产物; 和g。 从第二反应器中连续除去非水混溶性溶剂和重氮化合物的反应产物，以及适于进行这种方法的设备。