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    Aniline Type Compounds
    1.
    发明申请
    Aniline Type Compounds 有权
    苯胺类化合物

    公开(公告)号：US20140155451A1

    公开(公告)日：2014-06-05

    申请号：US14236362

    申请日：2012-08-10

    申请人： Karsten Koerber ,  Prashant Deshmukh ,  Florian Kaiser ,  Michael Rack ,  Timo Frasetto ,  Gemma Veitch ,  Markus Kordes ,  Marco Naujok

    发明人： Karsten Koerber ,  Prashant Deshmukh ,  Florian Kaiser ,  Michael Rack ,  Timo Frasetto ,  Gemma Veitch ,  Markus Kordes ,  Marco Naujok

    IPC分类号： A01N43/50 ,  A01N41/12

    CPC分类号： A01N43/56 ,  A01N37/28 ,  A01N41/12 ,  A01N43/50 ,  A01N43/80 ,  C07B2200/13 ,  C07C381/10 ,  C07D401/04 ,  C07D401/14 ,  C07D409/14 ,  C07D413/14

    摘要： The present invention relates to compounds of the formula (I) wherein R1 and R2 independently of one another are hydrogen, C1-C10-alkyl, C1-C10-haloalkyl, C3-C10-cycloalkyl, C3-C10-halocycloalkyl, C2-C10-alkenyl, C2-C10-haloalkenyl or together represent an aliphatic chain, or the like; R3 is halogen, cyano, C1-C8-alkyl, C1-C8-haloalkyl, C3-C8-cycloalkyl, C3-C8-halocycloalkyl, C2-C8-alkenyl, C2-C8-haloalkenyl, C1-C8-alkoxy, phenyl, or the like; R4 is hydrogen, C1-C10-alkyl, C1-C10-haloalkyl, C3-C8-cycloalkyl, C3-C8-halocycloalkyl, C2-C10-alkenyl, C2-C10-haloalkenyl, phenyl, or the like; t is 0 or 1; p is 0, 1, 2, 3 or 4. The present invention also relates to a process for preparing a compound of the formula (I) which comprises reacting a compound of the formula II with a compound of the formulae III or IV: where t, p, R1 R3, R3 and R4 are as defined in any of claims 1 to 6 and where A− is an equivalent of an anion having a pKB of at least 10 (determined under standard conditions in water).

    摘要翻译： 本发明涉及式（I）化合物，其中R 1和R 2彼此独立地是氢，C 1 -C 10 - 烷基，C 1 -C 10 - 卤代烷基，C 3 -C 10 - 环烷基，C 3 -C 10 - 卤代环烷基，C 2 -C 10 烯基，C 2 -C 10 - 卤代链烯基或一起代表脂族链等; R3是卤素，氰基，C1-C8-烷基，C1-C8-卤代烷基，C3-C8-环烷基，C3-C8-卤代环烷基，C2-C8-烯基，C2-C8-卤代烯基，C1-C8-烷氧基，苯基， 或类似物; R4是氢，C1-C10-烷基，C1-C10-卤代烷基，C3-C8-环烷基，C3-C8-卤代环烷基，C2-C10-烯基，C2-C10-卤代烯基，苯基等; t为0或1; 本发明还涉及制备式（I）化合物的方法，其包括使式II化合物与式III或IV化合物反应：其中 t，p，R 1，R 3，R 3和R 4如权利要求1至6中任一项所定义，其中A-是pKB为至少10（在水中标准条件下测定）的阴离子的当量。

    Aniline type compounds
    2.
    发明授权
    Aniline type compounds 有权
    苯胺型化合物

    公开(公告)号：US09006485B2

    公开(公告)日：2015-04-14

    申请号：US14236362

    申请日：2012-08-10

    申请人： Karsten Koerber ,  Prashant Deshmukh ,  Florian Kaiser ,  Michael Rack ,  Timo Frasetto ,  Gemma Veitch ,  Markus Kordes ,  Marco Naujok

    发明人： Karsten Koerber ,  Prashant Deshmukh ,  Florian Kaiser ,  Michael Rack ,  Timo Frasetto ,  Gemma Veitch ,  Markus Kordes ,  Marco Naujok

    IPC分类号： C07C313/00 ,  A01N41/12 ,  A01N43/50 ,  A01N43/56 ,  A01N43/80 ,  C07D401/04 ,  C07C381/10 ,  C07D401/14 ,  C07D413/14 ,  C07D409/14 ,  A01N37/28

    CPC分类号： A01N43/56 ,  A01N37/28 ,  A01N41/12 ,  A01N43/50 ,  A01N43/80 ,  C07B2200/13 ,  C07C381/10 ,  C07D401/04 ,  C07D401/14 ,  C07D409/14 ,  C07D413/14

    摘要： The present invention relates to compounds of the formula (I) wherein R1 and R2 independently of one another are hydrogen, C1-C10-alkyl, C1-C10-haloalkyl, C3-C10-cycloalkyl, C3-C10-halocycloalkyl, C2-C10-alkenyl, C2-C10-haloalkenyl or together represent an aliphatic chain, or the like; R3 is halogen, cyano, C1-C8-alkyl, C1-C8-haloalkyl, C3-C8-cycloalkyl, C3-C8-halocycloalkyl, C2-C8-alkenyl, C2-C8-haloalkenyl, C1-C8-alkoxy, phenyl, or the like; R4 is hydrogen, C1-C10-alkyl, C1-C10-haloalkyl, C3-C8-cycloalkyl, C3-C8-halocycloalkyl, C2-C10-alkenyl, C2-C10-haloalkenyl, phenyl, or the like; t is 0 or 1; p is 0, 1, 2, 3 or 4. The present invention also relates to a process for preparing a compound of the formula (I) which comprises reacting a compound of the formula II with a compound of the formulae III or IV: where t, p, R1 R3, R3 and R4 are as defined in any of claims 1 to 6 and where A− is an equivalent of an anion having a pKB of at least 10 (determined under standard conditions in water).

    摘要翻译： 本发明涉及式（I）化合物，其中R 1和R 2彼此独立地是氢，C 1 -C 10 - 烷基，C 1 -C 10 - 卤代烷基，C 3 -C 10 - 环烷基，C 3 -C 10 - 卤代环烷基，C 2 -C 10 烯基，C 2 -C 10 - 卤代链烯基或一起代表脂族链等; R3是卤素，氰基，C1-C8-烷基，C1-C8-卤代烷基，C3-C8-环烷基，C3-C8-卤代环烷基，C2-C8-烯基，C2-C8-卤代烯基，C1-C8-烷氧基，苯基， 或类似物; R4是氢，C1-C10-烷基，C1-C10-卤代烷基，C3-C8-环烷基，C3-C8-卤代环烷基，C2-C10-烯基，C2-C10-卤代烯基，苯基等; t为0或1; 本发明还涉及制备式（I）化合物的方法，其包括使式II化合物与式III或IV化合物反应：其中 t，p，R 1，R 3，R 3和R 4如权利要求1至6中任一项所定义，其中A-是pKB为至少10（在水中标准条件下测定）的阴离子的当量。

    Process for preparing N-substituted 1H-pyrazole-5-carbonylchloride compounds
    3.
    发明授权
    Process for preparing N-substituted 1H-pyrazole-5-carbonylchloride compounds 有权
    制备N-取代的1H-吡唑-5-碳酰氯化合物的方法

    公开(公告)号：US08921567B2

    公开(公告)日：2014-12-30

    申请号：US14235556

    申请日：2012-08-10

    申请人： Karsten Körber ,  Prashant Deshmukh ,  Florian Kaiser ,  Michael Rack ,  Timo Frassetto ,  Gemma Veitch ,  Markus Kordes

    发明人： Karsten Körber ,  Prashant Deshmukh ,  Florian Kaiser ,  Michael Rack ,  Timo Frassetto ,  Gemma Veitch ,  Markus Kordes

    IPC分类号： C07D401/04

    CPC分类号： C07D401/04

    摘要： The present invention relates to a process for preparing an N-substituted 1H-pyrazole-5-carbonylchloride compound of the formula (I) in which R1 is hydrogen, halogen, cyano, C1-C6-alkyl, C1-C6-fluoroalkyl, C3-C8-cycloalkyl, C3-C8-fluorocycloalkyl, C2-C6-alkenyl, C2-C6-fluoroalkenyl, C1-C6-alkoxy, C1-C6-fluoroalkoxy, C1-C4-fluoroalkoxy-C1-C4-alkyl, phenyl and the like; each R2 is independently selected from halogen, C1-C6-alkyl, C1-C6-fluoroalkyl, C3-C8-cycloalkyl, C3-C8-fluorocycloalkyl, C2-C6-alkenyl, C2-C6-fluoroalkenyl, C1-C6-alkoxy, phenyl and the like; r is 0, 1, 2, 3 or 4; comprising the steps of i) deprotonating a compound of the formula (II) in which the variables R1, R2 and r are each as defined above, with a base selected from lithium-organic base having a carbon or nitrogen bound lithium or with a magnesium-organic base having a carbon bound magnesium; and ii) subjecting the product obtained in step (i) to a chlorocarbonylation by reacting it with a reagent selected from the group consisting of phosgene or a phosgene equivalent, to obtain a compound of formula (I).

    摘要翻译： 本发明涉及制备式（I）的N-取代的1H-吡唑-5-碳酰氯化合物的方法，其中R1是氢，卤素，氰基，C1-C6-烷基，C1-C6-氟烷基，C3 C 1-8 - 环烷基，C 3 -C 8 - 氟代环烷基，C 2 -C 6 - 烯基，C 2 -C 6 - 氟烯基，C 1 -C 6 - 烷氧基，C 1 -C 6 - 氟烷氧基，C 1 -C 4 - 氟烷氧基-C 1 -C 4烷基，苯基和 喜欢; 每个R 2独立地选自卤素，C 1 -C 6 - 烷基，C 1 -C 6 - 氟代烷基，C 3 -C 8 - 环烷基，C 3 -C 8 - 氟代环烷基，C 2 -C 6 - 烯基，C 2 -C 6 - 氟烯基，C 1 -C 6烷氧基， 苯基等; r为0,1,2,3或4; 包括以下步骤：i）将其中变量R1，R2和r各自如上定义的式（II）化合物与选自具有碳或氮键合的锂的锂基或与镁结合的碱的碱 具有碳结合镁的无机碱; 和ii）通过使步骤（i）中获得的产物与选自光气或光气当量的试剂反应来进行氯羰化反应，得到式（I）化合物。

    Process for preparing N-substituted 1H-pyrazole-5-carbonylchloride compounds
    4.
    发明申请
    Process for preparing N-substituted 1H-pyrazole-5-carbonylchloride compounds 有权

    公开(公告)号：US20140163234A1

    公开(公告)日：2014-06-12

    申请号：US14235556

    申请日：2012-08-10

    申请人： Karsten Körber ,  Prashant Deshmukh ,  Florian Kaiser ,  Michael Rack ,  Timo Frassetto ,  Gemma Veitch ,  Markus Kordes

    发明人： Karsten Körber ,  Prashant Deshmukh ,  Florian Kaiser ,  Michael Rack ,  Timo Frassetto ,  Gemma Veitch ,  Markus Kordes

    IPC分类号： C07D401/04

    CPC分类号： C07D401/04

    摘要： The present invention relates to a process for preparing an N-substituted 1H-pyrazole-5-carbonylchloride compound of the formula (I) in which R1 is hydrogen, halogen, cyano, C1-C6-alkyl, C1-C6-fluoroalkyl, C3-C8-cycloalkyl, C3-C8-fluorocycloalkyl, C2-C6-alkenyl, C2-C6-fluoroalkenyl, C1-C6-alkoxy, C1-C6-fluoroalkoxy, C1-C4-fluoroalkoxy-C1-C4-alkyl, phenyl and the like; each R2 is independently selected from halogen, C1-C6-alkyl, C1-C6-fluoroalkyl, C3-C8-cycloalkyl, C3-C8-fluorocycloalkyl, C2-C6-alkenyl, C2-C6-fluoroalkenyl, C1-C6-alkoxy, phenyl and the like; r is 0, 1, 2, 3 or 4; comprising the steps of i) deprotonating a compound of the formula (II) in which the variables R1, R2 and r are each as defined above, with a base selected from lithium-organic base having a carbon or nitrogen bound lithium or with a magnesium-organic base having a carbon bound magnesium; and ii) subjecting the product obtained in step (i) to a chlorocarbonylation by reacting it with a reagent selected from the group consisting of phosgene or a phosgene equivalent, to obtain a compound of formula (I).

    Process for preparing substituted isoxazoline compounds and their precursors
    8.
    发明授权
    Process for preparing substituted isoxazoline compounds and their precursors 有权
    取代异恶唑啉化合物及其前体的制备方法

    公开(公告)号：US08853410B2

    公开(公告)日：2014-10-07

    申请号：US13266265

    申请日：2010-04-29

    申请人： Michael Rack ,  Karsten Koerber ,  Florian Kaiser

    发明人： Michael Rack ,  Karsten Koerber ,  Florian Kaiser

    IPC分类号： C07D413/12 ,  C07D413/04

    CPC分类号： C07D413/04

    摘要： The present invention relates to a new method of preparing halogenated styrene compounds of formula (VIII) which are precursors in the process of synthesis of substituted isoxazoline compounds of formula (I) wherein R1 to R5, R8 and R9 are described as in the description. The present invention relates further to the synthesis of compounds of formula (I) starting from acetophenones. The desired styrenes of formula are prepared from the appropriate substituted acetophenone. Asides bromo anilines react with formoxime. Obtained oximes undergo a cycloaddition with the styrenes and give isoxazolines. Compounds of formula (I) can then be prepared in a palladium catalyzed carbonylative amination reaction of the isoxazolines.

    摘要翻译： 本发明涉及一种制备式（Ⅷ）卤代苯乙烯化合物的新方法，它是在合成式（I）的取代的异恶唑啉化合物的方法中的前体，其中R1至R5，R8和R9如说明书所述。 本发明还涉及从苯乙酮开始合成式（I）化合物。 所需的配方苯乙烯由合适的取代苯乙酮制备。 溴代苯胺与甲肟反应。 获得的肟与苯乙烯进行环加成并得到异恶唑啉。 然后可以在异恶唑啉的钯催化的羰基化胺化反应中制备式（I）化合物。

    Process for Preparing Substituted Isoxazoline Compounds and Their Precursors
    9.
    发明申请
    Process for Preparing Substituted Isoxazoline Compounds and Their Precursors 有权
    制备取代的异恶唑啉化合物及其前体的方法

    公开(公告)号：US20120059171A1

    公开(公告)日：2012-03-08

    申请号：US13266265

    申请日：2010-04-29

    申请人： Michael Rack ,  Karsten Koerber ,  Florian Kaiser

    发明人： Michael Rack ,  Karsten Koerber ,  Florian Kaiser

    IPC分类号： C07D413/12

    CPC分类号： C07D413/04

    摘要： The present invention relates to a new method of preparing halogenated styrene compounds of formula (VIII) which are precursors in the process of synthesis of substituted isoxazoline compounds of formula (I) wherein R1 to R5, R8 and R9 are described as in the description.The present invention relates further to the synthesis of compounds of formula (I) starting from acetophenones. The desired styrenes of formula are prepared from the appropriate substituted acetophenone. Asides bromo anilines react with formoxime. Obtained oximes undergo a cycloaddition with the styrenes and give isoxazolines. Compounds of formula (I) can then be prepared in a palladium catalyzed carbonylative amination reaction of the isoxazolines.

    摘要翻译： 本发明涉及一种制备式（Ⅷ）卤代苯乙烯化合物的新方法，它是在合成式（I）的取代的异恶唑啉化合物的方法中的前体，其中R1至R5，R8和R9如说明书所述。 本发明还涉及从苯乙酮开始合成式（I）化合物。 所需的配方苯乙烯由合适的取代苯乙酮制备。 溴代苯胺与甲肟反应。 获得的肟与苯乙烯进行环加成并得到异恶唑啉。 然后可以在异恶唑啉的钯催化的羰基化胺化反应中制备式（I）化合物。