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。

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).

公开(公告)号：US08563474B2

公开(公告)日：2013-10-22

申请号：US13003037

申请日：2009-07-06

申请人： Karsten Koerber ,  Florian Kaiser ,  Juergen Langewald

发明人： Karsten Koerber ,  Florian Kaiser ,  Juergen Langewald

IPC分类号： A01N43/80 ,  A01N43/56 ,  A01P7/04

CPC分类号： A01N43/88 ,  A01N43/40 ,  A01N43/50 ,  A01N43/80 ,  A01N43/90 ,  A01N53/00 ,  A61K31/277 ,  A61K31/42 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/455 ,  A61K31/5395 ,  A61K31/7048 ,  A01N51/00 ,  A01N2300/00

摘要： The present invention relates to pesticidal mixtures comprising as active compounds 1) at least one isoaxazoline compound I of the formula (I) wherein R1, R2, R3, R4, R5 and A are defined in the description; and 2) at least one active compound II selected from a group A comprising acteylcholine esterase inhibitors, GABA-gated chloride channel antagonists, sodium channel modulators, nicotinic acteylcholine receptor agonists/antagonists, chloride channel activators, juvenile hormone mimics, compounds affecting the oxidative phosphorylation, inhibitors of the chitin biosynthesis, moulting disruptors, inhibitors of the MET, voltage-dependent sodium channel blockers, inhibitors of the lipid synthesis and other compounds as defined in the description, in synergistically effective amounts. The invention relates further to methods and use of these mixtures for combating insects, arachnids or nematodes in and on plants, and for protecting such plants being infested with pests, especially also for protecting plant propagation material as like seeds.

摘要翻译： 本发明涉及包含作为活性化合物的杀虫混合物1）至少一种式（I）的异唑啉化合物I，其中R 1，R 2，R 3，R 4，R 5和A在说明书中定义; 和2）选自包含活性胆碱酯酶抑制剂，GABA门控氯化物通道拮抗剂，钠通道调节剂，烟碱型活性胆碱受体激动剂/拮抗剂，氯化物通道激活剂，幼年激素模拟物，影响氧化磷酸化的化合物的组A中的至少一种活性化合物II ，甲壳素生物合成抑制剂，蜕皮破坏剂，MET抑制剂，电压依赖性钠通道阻滞剂，脂质合成抑制剂和描述中定义的其它化合物，具有协同有效量。 本发明还涉及这些混合物用于防治植物内和植物上的昆虫，蜘蛛或线虫的方法和用途，以及用于保护被害虫侵染的植物，特别是用于保护植物繁殖材料如同种子。

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。

公开(公告)号：US08597688B2

公开(公告)日：2013-12-03

申请号：US13003032

申请日：2009-07-02

申请人： Karsten Koerber ,  Florian Kaiser ,  Egon Haden

发明人： Karsten Koerber ,  Florian Kaiser ,  Egon Haden

IPC分类号： A01N59/26 ,  A61K33/42

CPC分类号： A01N43/80 ,  A01N37/24 ,  A01N37/50 ,  A01N43/40 ,  A01N43/54 ,  A01N43/653 ,  A01N43/88 ,  A01N47/12 ,  A01N47/14 ,  A01N47/18 ,  A01N47/24 ,  A01N47/38 ,  A01N2300/00

摘要： The present invention relates to pesticidal mixtures comprising as active components 1) at least one isoxazoline compound I of the formula I wherein R1, R2, R3, R4, R5 and A are defined as in the description; and 2) at least one fungicidal compounds II selected from azoles, strobilurins, carboxamides, carbamates, heterocyclic and various other compounds as defined in the description, in synergistically effective amounts. The invention relates further to methods and use of these mixtures for combating insects, arachnids or nematodes and harmful fungis in and on plants, and for protecting such plants being infested with pests, especially also for protecting seeds.

摘要翻译： 本发明涉及包含作为活性组分的杀虫混合物1）至少一种式I的异恶唑啉化合物I，其中R 1，R 2，R 3，R 4，R 5和A如描述中所定义; 和2）协同有效量的至少一种选自吡咯，嗜球半胱氨酸，羧酰胺，氨基甲酸酯，杂环和各种其它如描述中定义的其它化合物的杀真菌化合物II。 本发明还涉及这些混合物用于防治昆虫，蜘蛛或线虫和植物中和植物上的有害真菌的方法和用途，并且用于保护被害虫侵染的植物，特别是用于保护种子。

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。

公开(公告)号：US20110159107A1

公开(公告)日：2011-06-30

申请号：US13003032

申请日：2009-07-02

申请人： Karsten Koerber ,  Florian Kaiser ,  Egon Haden

发明人： Karsten Koerber ,  Florian Kaiser ,  Egon Haden

IPC分类号： A01N43/80 ,  A01N55/10 ,  A01N43/40 ,  A01N43/90 ,  A01N43/54 ,  A01N43/88 ,  A01N43/78 ,  A01N43/84 ,  A01N43/76 ,  A01N59/26 ,  A01P7/04 ,  A01P3/00 ,  A01P5/00 ,  A01P7/00

CPC分类号： A01N43/80 ,  A01N37/24 ,  A01N37/50 ,  A01N43/40 ,  A01N43/54 ,  A01N43/653 ,  A01N43/88 ,  A01N47/12 ,  A01N47/14 ,  A01N47/18 ,  A01N47/24 ,  A01N47/38 ,  A01N2300/00

摘要： The present invention relates to pesticidal mixtures comprising as active components 1) at least one isoxazoline compound I of the formula I wherein R1, R2, R3, R4, R5 and A are defined as in the description; and 2) at least one fungicidal compounds II selected from azoles, strobilurins, carboxamides, carbamates, heterocyclic and various other compounds as defined in the description, in synergistically effective amounts. The invention relates further to methods and use of these mixtures for combating insects, arachnids or nematodes and harmful fungis in and on plants, and for protecting such plants being infested with pests, especially also for protecting seeds.

摘要翻译： 本发明涉及包含作为活性组分的杀虫混合物1）至少一种式I的异恶唑啉化合物I，其中R 1，R 2，R 3，R 4，R 5和A如描述中所定义; 和2）协同有效量的至少一种选自吡咯，嗜球半胱氨酸，羧酰胺，氨基甲酸酯，杂环和各种其它如描述中定义的其它化合物的杀真菌化合物II。 本发明还涉及这些混合物用于防治昆虫，蜘蛛或线虫和植物中和植物上的有害真菌的方法和用途，并且用于保护被害虫侵染的植物，特别是用于保护种子。

公开(公告)号：US20110118212A1

公开(公告)日：2011-05-19

申请号：US13003037

申请日：2009-07-06

申请人： Karsten Koerber ,  Florian Kaiser ,  Juergen Langewald

发明人： Karsten Koerber ,  Florian Kaiser ,  Juergen Langewald

IPC分类号： A01N57/16 ,  A01N43/80 ,  A01N43/40 ,  A01N43/78 ,  A01N43/54 ,  A01N43/16 ,  A01N43/24 ,  A01P15/00 ,  A61K31/42 ,  A61K31/44 ,  A61K31/426 ,  A61K31/505 ,  A61K31/675 ,  A61K31/465 ,  A61K31/715 ,  A61K31/4439 ,  A61P33/00 ,  A61P33/14

CPC分类号： A01N43/88 ,  A01N43/40 ,  A01N43/50 ,  A01N43/80 ,  A01N43/90 ,  A01N53/00 ,  A61K31/277 ,  A61K31/42 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/455 ,  A61K31/5395 ,  A61K31/7048 ,  A01N51/00 ,  A01N2300/00

摘要： The present invention relates to pesticidal mixtures comprising as active compounds 1) at least one isoaxazoline compound I of the formula (I) wherein R1, R2, R3, R4, R5 and A are defined in the description; and 2) at least one active compound II selected from a group A comprising acteylcholine esterase inhibitors, GABA-gated chloride channel antagonists, sodium channel modulators, nicotinic acteylcholine receptor agonists/antagonists, chloride channel activators, juvenile hormone mimics, compounds affecting the oxidative phosphorylation, inhibitors of the chitin biosynthesis, moulting disruptors, inhibitors of the MET, voltage-dependent sodium channel blockers, inhibitors of the lipid synthesis and other compounds as defined in the description, in synergistically effective amounts. The invention relates further to methods and use of these mixtures for combating insects, arachnids or nematodes in and on plants, and for protecting such plants being infested with pests, especially also for protecting plant propagation material as like seeds.

摘要翻译： 本发明涉及包含作为活性化合物的杀虫混合物1）至少一种式（I）的异唑啉化合物I，其中R 1，R 2，R 3，R 4，R 5和A在说明书中定义; 和2）选自包含活性胆碱酯酶抑制剂，GABA门控氯化物通道拮抗剂，钠通道调节剂，烟碱型活性胆碱受体激动剂/拮抗剂，氯化物通道激活剂，幼年激素模拟物，影响氧化磷酸化的化合物的组A中的至少一种活性化合物II ，甲壳素生物合成抑制剂，蜕皮破坏剂，MET抑制剂，电压依赖性钠通道阻滞剂，脂质合成抑制剂和描述中定义的其它化合物，具有协同有效量。 本发明还涉及这些混合物用于防治植物内和植物上的昆虫，蜘蛛或线虫的方法和用途，以及用于保护被害虫侵染的植物，特别是用于保护植物繁殖材料如同种子。

公开(公告)号：US20140200136A1

公开(公告)日：2014-07-17

申请号：US14241270

申请日：2012-08-31

申请人： Florian Kaiser ,  Steffen Gross ,  Egon Haden ,  Arun Narine

发明人： Florian Kaiser ,  Steffen Gross ,  Egon Haden ,  Arun Narine

IPC分类号： A01N43/54 ,  A01N37/50 ,  A01N43/40 ,  A01N43/50 ,  A01N43/52 ,  A01N37/34 ,  A01N43/88 ,  A01N43/56 ,  A01N47/14 ,  A01N47/24

CPC分类号： A01N43/54 ,  A01N37/34 ,  A01N37/50 ,  A01N43/40 ,  A01N43/50 ,  A01N43/52 ,  A01N43/56 ,  A01N43/88 ,  A01N47/14 ,  A01N47/24 ,  A01N47/18 ,  A01N2300/00

摘要： The present invention relates to pesticidal mixtures comprising as active compounds1) at least one pesticidal active 3-arylquinazolin-4-one compound I of formula (I): wherein R1, R2, R3, R4, k and n are defined in the description; and 2) at least one fungicidal compounds II selected from azoles, strobilurins, carboxamides, carbamates, heterocyclic and various other compounds as defined in the description, in synergistically effective amounts.The invention relates further to methods and use of these mixtures for combating insects, arachnids or nematodes and harmful fungis in and on plants, and for protecting such plants being infested with pests, especially also for protecting seeds.

摘要翻译： 本发明涉及包含作为活性化合物的杀虫混合物1）至少一种式（I）的杀虫活性3-芳基喹唑啉-4-酮化合物I：其中R1，R2，R3，R4，k和n在说明书中定义 ; 和2）协同有效量的至少一种选自吡咯，嗜球脑炎，羧酰胺，氨基甲酸酯，杂环和各种其它化合物的杀真菌化合物II。 本发明还涉及这些混合物用于防治昆虫，蜘蛛或线虫和植物中和植物上的有害真菌的方法和用途，并且用于保护被害虫侵染的植物，特别是用于保护种子。

公开(公告)号：US20140213445A1

公开(公告)日：2014-07-31

申请号：US14241262

申请日：2012-08-31

申请人： Florian Kaiser ,  Steffen Gross ,  Arun Narine ,  Koshi Gunjima

发明人： Florian Kaiser ,  Steffen Gross ,  Arun Narine ,  Koshi Gunjima

IPC分类号： A01N43/54

CPC分类号： A01N43/54 ,  A01N25/00

摘要： The present invention relates to agricultural methods and the use of 3-arylquinazolin-4-one derivatives of formula (I) wherein R1, R2, R3, R4, k and n are defined in the description in soil application methods.The compounds of the formula (I) are highly suitable for controlling animal pests such as insects and/or spider mites and/or nematodes by treating the soil/growth substrate by drenching or drip application or dipping or soil injection.

摘要翻译： 本发明涉及农业方法和式（I）的3-芳基喹唑啉-4-酮衍生物的用途，其中R1，R2，R3，R4，k和n在土壤施用方法的描述中定义。 式（I）的化合物通过浸渍或滴灌或浸渍或土壤注射处理土壤/生长底物，非常适合于防治动物害虫如昆虫和/或蜘蛛螨和/或线虫。