公开(公告)号：US08115012B2

公开(公告)日：2012-02-14

申请号：US12513003

申请日：2007-11-02

申请人： Martin Sukopp ,  Michael Rack ,  Sebastian Peer Smidt ,  Sandra Löhr ,  Michael Keil ,  Jochen Dietz ,  Joachim Rheinheimer ,  Thomas Grote ,  Thomas Zierke ,  Jan Klaas Lohmann

发明人： Martin Sukopp ,  Michael Rack ,  Sebastian Peer Smidt ,  Sandra Löhr ,  Michael Keil ,  Jochen Dietz ,  Joachim Rheinheimer ,  Thomas Grote ,  Thomas Zierke ,  Jan Klaas Lohmann

IPC分类号： C07D231/10 ,  C07F7/08

CPC分类号： C07D231/14

摘要： The present invention relates to a process for preparing difluoromethyl-substituted pyrazol-4-ylcarboxylates of the formula I in which R1 is C1-C8-alkyl, C3-C8-cycloalkyl, C1-C4-alkoxy-C1-C4-alkyl, etc.; and R2 is hydrogen, C1-C4-alkyl, benzyl or phenyl, wherein a) a compound of the general formula II in which X is fluorine, chlorine or bromine, R1 has one of the meanings given above and R4 is C1-C8-alkyl, C3-C8-cycloalkyl, C2-C8-alkenyl, benzyl or phenyl, is reacted with a silane compound of the general formula R3nSiCl(4-n) in which n is 1, 2 or 3 and the substituents R3 are independently of one another selected from the group consisting of C1-C8-alkyl and phenyl and with a metal selected from the metals of groups 1, 2, 3, 4 and 12 of the Periodic Table of the Elements having a redox potential of less than −0.7 V, based on a normal hydrogen electrode (at 25° C. and 101.325 kPa); and b) the reaction mixture from step a) is reacted with a compound of the general formula III R2HN—NH2  (III) in which R2 has one of the meanings given above.

摘要翻译： 本发明涉及制备式Ⅰ的二氟甲基取代的吡唑-4-基羧酸酯的方法，其中R 1是C 1 -C 8烷基，C 3 -C 8环烷基，C 1 -C 4烷氧基-C 1 -C 4烷基等 。 R 2是氢，C 1 -C 4 - 烷基，苄基或苯基，其中a）通式II的化合物，其中X是氟，氯或溴，R 1具有上面给出的含义之一，R 4是C 1 -C 8 - 烷基，C 3 -C 8 - 环烷基，C 2 -C 8 - 烯基，苄基或苯基与通式R 3 n SiCl（4-n）的硅烷化合物反应，其中n为1,2或3，取代基R 3独立地为 选自由C 1 -C 8 - 烷基和苯基组成的组中的一种，以及选自元素周期表第1,2,3,4和12族金属的金属，其氧化还原电位小于-0.7 V，基于正常的氢电极（在25℃和101.325kPa）; 和b）将来自步骤a）的反应混合物与通式III的化合物R2HN-NH2（III）反应，其中R2具有上述含义之一。

公开(公告)号：US20100069646A1

公开(公告)日：2010-03-18

申请号：US12513003

申请日：2007-11-02

申请人： Martin Sukopp ,  Michael Rack ,  Sebastian Peer Smidt ,  Sandra Löhr ,  Michael Keil ,  Jochen Dietz ,  Joachim Rheinheimer ,  Thomas Grote ,  Thomas Zierke ,  Jan Klaas Lohmann

发明人： Martin Sukopp ,  Michael Rack ,  Sebastian Peer Smidt ,  Sandra Löhr ,  Michael Keil ,  Jochen Dietz ,  Joachim Rheinheimer ,  Thomas Grote ,  Thomas Zierke ,  Jan Klaas Lohmann

IPC分类号： C07D231/10 ,  C07F7/08

CPC分类号： C07D231/14

摘要： The present invention relates to a process for preparing difluoromethyl-substituted pyrazol-4-ylcarboxylates of the formula I in which R1 is C1-C8-alkyl, C3-C8-cycloalkyl, C1-C4-alkoxy-C1-C4-alkyl, etc.; and R2 is hydrogen, C1-C4-alkyl, benzyl or phenyl, wherein a) a compound of the general formula II in which X is fluorine, chlorine or bromine, R1 has one of the meanings given above and R4 is C1-C8-alkyl, C3-C8-cycloalkyl, C2-C8-alkenyl, benzyl or phenyl, is reacted with a silane compound of the general formula R3nSiCl(4-n) in which n is 1, 2 or 3 and the substituents R3 are independently of one another selected from the group consisting of C1-C8-alkyl and phenyl and with a metal selected from the metals of groups 1, 2, 3, 4 and 12 of the Periodic Table of the Elements having a redox potential of less than −0.7 V, based on a normal hydrogen electrode (at 25° C. and 101.325 kPa); and b) the reaction mixture from step a) is reacted with a compound of the general formula III R2HN—NH2   (III) in which R2 has one of the meanings given above.

摘要翻译： 本发明涉及制备式Ⅰ的二氟甲基取代的吡唑-4-基羧酸酯的方法，其中R 1是C 1 -C 8烷基，C 3 -C 8环烷基，C 1 -C 4烷氧基-C 1 -C 4烷基等 。 并且R 2是氢，C 1 -C 4 - 烷基，苄基或苯基，其中a）通式II的化合物，其中X是氟，氯或溴，R 1具有上面给出的含义之一，R 4是C 1 -C 8 - 烷基，C 3 -C 8 - 环烷基，C 2 -C 8 - 烯基，苄基或苯基与通式R 3 n SiCl（4-n）的硅烷化合物反应，其中n为1,2或3，取代基R 3独立地为 选自由C 1 -C 8 - 烷基和苯基组成的组中的一种，以及选自元素周期表第1,2,3,4和12族金属的金属，其氧化还原电位小于-0.7 V，基于正常的氢电极（在25℃和101.325kPa）; 和b）将来自步骤a）的反应混合物与通式III的化合物R2HN-NH2（III）反应，其中R2具有上述含义之一。

公开(公告)号：US20110172436A1

公开(公告)日：2011-07-14

申请号：US12990340

申请日：2009-05-04

申请人： Bernd Wolf ,  Volker Maywald ,  Michael Keil ,  Christopher Koradin ,  Michael Rack ,  Thomas Zierke ,  Martin Sukopp

发明人： Bernd Wolf ,  Volker Maywald ,  Michael Keil ,  Christopher Koradin ,  Michael Rack ,  Thomas Zierke ,  Martin Sukopp

IPC分类号： C07D231/14 ,  C07C243/10

CPC分类号： C07D409/12 ,  C07C251/76 ,  C07C251/84 ,  C07C251/86 ,  C07D231/14

摘要： The invention provides an Ethernet bridge or router comprising a network fabric adapted to provide interconnectivity to a plurality of Ethernet ports, each of the Ethernet ports being adapted to receive and/or transmit Ethernet frames, and wherein the Ethernet bridge or router further comprises an encapsulator connected to receive Ethernet Protocol Data Units from the Ethernet ports, wherein the encapsulator is operable to generate a Fabric Protocol Data Unit from a received Ethernet Protocol Data Unit, the Fabric Protocol Data Unit comprising a header portion, and a payload portion which comprises the Ethernet Protocol Data Unit concerned, and wherein the encapsulator is operable to transform Ethernet destination address information from the Ethernet Protocol Data Unit into a routing definition for the network fabric, and to include this routing definition in the header portion of the Fabric Protocol Data Unit. Also provided is a method of data delivery across a network.

摘要翻译： 本发明提供了一种以太网桥或路由器，其包括适于提供与多个以太网端口的互连性的网络结构，每个以太网端口适于接收和/或发送以太网帧，并且其中所述以太网桥或路由器还包括封装器 连接以从以太网端口接收以太网协议数据单元，其中所述封装器可操作以从接收到的以太网协议数据单元生成结构协议数据单元，所述结构协议数据单元包括报头部分和包括以太网的有效载荷部分 协议数据单元，并且其中所述封装器可操作以将以太网目的地地址信息从以太网协议数据单元转换为所述网络结构的路由定义，并将所述路由定义包括在所述结构协议数据单元的报头部分中。 还提供了一种通过网络进行数据传送的方法。

公开(公告)号：US08598222B2

公开(公告)日：2013-12-03

申请号：US12990340

申请日：2009-05-04

申请人： Bernd Wolf ,  Volker Maywald ,  Michael Keil ,  Christopher Koradin ,  Michael Rack ,  Thomas Zierke ,  Martin Sukopp

发明人： Bernd Wolf ,  Volker Maywald ,  Michael Keil ,  Christopher Koradin ,  Michael Rack ,  Thomas Zierke ,  Martin Sukopp

IPC分类号： A61K31/415 ,  C07D231/14

CPC分类号： C07D409/12 ,  C07C251/76 ,  C07C251/84 ,  C07C251/86 ,  C07D231/14

摘要： The present invention relates to a process for preparing 1,3-substituted pyrazole compounds of the formula I in which X is especially a CX1X2X3 group in which X1, X2 and X3 are each independently especially hydrogen, fluorine or chlorine, R1 is C1-C4-alkyl or cyclopropyl, and R2 is hydrogen, CN or a CO2R2a group in which R2a is especially C1-C6-alkyl, comprising the following steps: i) reacting a compound of the formula II with a hydrazone of the formula III where the variables X and R2 in formula II are each as defined for formula I, Y is oxygen, an NRy1 group or an [NRy2Ry3]+Z− group, R3 is OR3a or an NR3bR3c group, and where the variable R1 in formula III is as defined for formula I, R4 and R5 are each independently hydrogen, C1-C6-alkyl, optionally substituted phenyl, where at least one of the R4 and R5 radicals is different from hydrogen, and where R4 and R5 together with the carbon atom to which they are bonded may also be a 5- to 10-membered saturated carbocycle; ii) treating the reaction product obtained with an acid in the presence of water.

摘要翻译： 本发明涉及一种制备式I的1,3-取代吡唑化合物的方法，其中X特别是X 1，X 2和X 3各自独立地是氢，氟或氯，R 1是C 1 -C 4 - 烷基或环丙基，并且R 2是氢，CN或其中R 2a特别是C 1 -C 6 - 烷基的CO 2 R 2 a基团，包括以下步骤：i）使式II化合物与式III的腙反应，其中变量 式II中的X和R 2各自如式I所定义，Y是氧，NRy1基或[NRy2Ry3] + Z-基，R3是OR3a或NR3bR3c基团，其中式III中的变量R1如所定义 对于式I，R 4和R 5各自独立地为氢，C 1 -C 6 - 烷基，任选取代的苯基，其中R 4和R 5基团中的至少一个不同于氢，并且其中R 4和R 5与它们的碳原子一起 键也可以是5至10元饱和碳环; ii）在水存在下用酸处理反应产物。

公开(公告)号：US20110190510A1

公开(公告)日：2011-08-04

申请号：US13121973

申请日：2009-09-28

申请人： Martin Sukopp ,  Alexander Korte ,  Stefan Fülster ,  Michael Keil ,  Michael Rack

发明人： Martin Sukopp ,  Alexander Korte ,  Stefan Fülster ,  Michael Keil ,  Michael Rack

IPC分类号： C07D231/44 ,  C07C313/04 ,  B01D3/36

CPC分类号： C07D231/44 ,  C07C313/04

摘要： The invention relates to a process for purifying trifluoromethanesulfinic acid by azeotropic distillation with an aromatic solvent, to processes for preparing purified trifluoromethanesulfinic acid and to the use of the purified trifluoronnethanesulfinic acid for preparing trifluoromethylsulfinylated pyrazole derivatives, especially fipronil.

摘要翻译： 本发明涉及一种通过与芳族溶剂共沸蒸馏纯化三氟甲磺酸的方法，以及用于制备纯化的三氟甲磺酸的方法，以及使用纯化的三氟甲磺酰亚胺制备三氟甲基亚硫酰化的吡唑衍生物，特别是氟虫腈。

公开(公告)号：US08354007B2

公开(公告)日：2013-01-15

申请号：US13121973

申请日：2009-09-28

申请人： Martin Sukopp ,  Alexander Korte ,  Stefan Fülster ,  Michael Keil ,  Michael Rack

发明人： Martin Sukopp ,  Alexander Korte ,  Stefan Fülster ,  Michael Keil ,  Michael Rack

IPC分类号： B01D3/36 ,  C07D231/10 ,  C07C313/02

CPC分类号： C07D231/44 ,  C07C313/04

摘要： The invention relates to a process for purifying trifluoromethanesulfinic acid by azeotropic distillation with an aromatic solvent, to processes for preparing purified trifluoromethanesulfinic acid and to the use of the purified trifluoronnethanesulfinic acid for preparing trifluoromethylsulfinylated pyrazole derivatives, especially fipronil.

摘要翻译： 本发明涉及一种通过与芳族溶剂共沸蒸馏纯化三氟甲磺酸的方法，以及用于制备纯化的三氟甲磺酸的方法，以及使用纯化的三氟甲磺酰亚胺制备三氟甲基亚硫酰化的吡唑衍生物，特别是氟虫腈。

公开(公告)号：US20100093822A1

公开(公告)日：2010-04-15

申请号：US12514103

申请日：2007-11-05

申请人： Martin Sukopp ,  Oliver Kuhn ,  Carsten Gröning ,  Michael Keil ,  Jon J. Longlet

发明人： Martin Sukopp ,  Oliver Kuhn ,  Carsten Gröning ,  Michael Keil ,  Jon J. Longlet

IPC分类号： C07D231/44 ,  A01N43/56 ,  A01P5/00 ,  A01P7/02 ,  A01P7/04 ,  A61K31/415 ,  A61P33/00

CPC分类号： C07D231/44 ,  A01N43/56

摘要： The present invention relates to a process for the sulfinylation of a pyrazole derivative, characterized in that 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-1H-pyrazole-3-carbonitrile (II) is reacted with a sulfinylating agent S in the presence of at least one amine acid complex wherein the amine(s) are selected from cyclic secondary amines and the acid(s) are selected from sulfonic acid derivatives, and with the addition of a halogenating agent, wherein S is [CF3S(O)]2O; or CF3S(O)X wherein X means fluoro, chloro, bromo, iodo, a hydroxy group, or an alkaline or alkaline earth metal salt of the hydroxy group; or mixtures thereof.

摘要翻译： 本发明涉及吡唑衍生物亚硫酰化的方法，其特征在于5-氨基-1- [2,6-二氯-4-（三氟甲基）苯基] -1H-吡唑-3-甲腈（II）是 在至少一种胺酸络合物存在下与亚硫酰化剂S反应，其中胺选自环状仲胺，酸选自磺酸衍生物，并且通过加入卤化剂， 其中S是[CF 3 S（O）] 2 O; 或CF 3 S（O）X，其中X表示氟，氯，溴，碘，羟基或羟基的碱金属或碱土金属盐; 或其混合物。

公开(公告)号：US20100137395A1

公开(公告)日：2010-06-03

申请号：US12514098

申请日：2007-11-05

申请人： Martin Sukopp ,  Oliver Kuhn ,  Carstein Gröning ,  Michael Keil ,  Jon J. Longlet

发明人： Martin Sukopp ,  Oliver Kuhn ,  Carstein Gröning ,  Michael Keil ,  Jon J. Longlet

IPC分类号： A01N43/56 ,  A01P7/04 ,  A01P7/02 ,  A01P5/00 ,  A61K31/415 ,  A61P33/00 ,  C07D231/44

CPC分类号： C07D231/44

摘要： The present invention relates to a process for the sulfinylation of a pyrazole derivative, characterized in that 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-1H-pyrazole-3-carbonitrile (II) is reacted with a sulfinylating agent selected from trifluoromethylsulfinic acid, trifluoromethylsulfinic acid anhydride, and a trifluoromethylsulfinate alkaline or alkaline earth metal salt and mixtures of the acid and/or the salt(s), in the presence of at least one amine acid complex wherein the amine(s) are selected from tertiary amines and the acid(s) are selected from hydrofluoric, hydrochloric, hydrobromic and hydroiodic acid and sulfonic acid derivatives, and with the addition of a halogenating agent.

摘要翻译： 本发明涉及吡唑衍生物亚硫酰化的方法，其特征在于5-氨基-1- [2,6-二氯-4-（三氟甲基）苯基] -1H-吡唑-3-甲腈（II）是 与选自三氟甲基亚磺酸，三氟甲基亚磺酸酐和三氟甲基亚硫酸盐碱金属或碱土金属盐的亚磺酰化剂以及酸和/或盐的混合物在至少一种胺酸络合物的存在下反应，其中胺 选自叔胺，酸选自氢氟酸，盐酸，氢溴酸和氢碘酸以及磺酸衍生物，并加入卤化剂。

公开(公告)号：US20100004307A1

公开(公告)日：2010-01-07

申请号：US12514109

申请日：2007-11-05

申请人： Martin Sukopp ,  Oliver Kuhn ,  Carsten Gröning ,  Michael Keil ,  Jon J. Longlet

发明人： Martin Sukopp ,  Oliver Kuhn ,  Carsten Gröning ,  Michael Keil ,  Jon J. Longlet

IPC分类号： A01N43/56 ,  C07D231/38 ,  C09K3/00 ,  A01P5/00

CPC分类号： C07D231/44 ,  A01N43/56 ,  A01N47/02

摘要： The present invention relates to a process for the sulfinylation of a pyrazole derivative, characterized in that 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-1H-pyrazole-3-carbonitrile (II) is reacted with a sulfinylating agent S in the presence of at least one amine acid complex wherein the amine(s) are selected from secondary and/or tertiary amines and the acid(s) are selected from hydrofluoric, hydrochloric, hydrobromic and hydroiodic acid and sulfonic acid derivatives, and with the addition of a halogenating agent, wherein S is [CF3S(O)]2O; or CF3S(O)X wherein X means fluoro, chloro, bromo, iodo, a hydroxy group, or an alkaline or alkaline earth metal salt of the hydroxy group; or mixtures thereof, wherein the temperature of the reaction mixture at no time exceeds 39° C.

摘要翻译： 本发明涉及吡唑衍生物亚硫酰化的方法，其特征在于5-氨基-1- [2,6-二氯-4-（三氟甲基）苯基] -1H-吡唑-3-甲腈（II）是 在至少一种胺酸配合物存在下与亚硫酰化剂S反应，其中胺选自仲胺和/或叔胺，酸选自氢氟酸，盐酸，氢溴酸和氢碘酸和磺酸 并且加入卤化剂，其中S是[CF 3 S（O）] 2 O; 或CF 3 S（O）X，其中X表示氟，氯，溴，碘，羟基或羟基的碱金属或碱土金属盐; 或其混合物，其中反应混合物的温度在任何时候都不超过39℃。

公开(公告)号：US08629287B2

公开(公告)日：2014-01-14

申请号：US12514103

申请日：2007-11-05

申请人： Martin Sukopp ,  Oliver Kuhn ,  Carsten Gröning ,  Michael Keil ,  Jon J. Longlet

发明人： Martin Sukopp ,  Oliver Kuhn ,  Carsten Gröning ,  Michael Keil ,  Jon J. Longlet

IPC分类号： C07D231/18

CPC分类号： C07D231/44 ,  A01N43/56

摘要： The present invention relates to a process for the sulfinylation of a pyrazole derivative, characterized in that 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-1H-pyrazole-3-carbonitrile (II) is reacted with a sulfinylating agent S in the presence of at least one amine acid complex wherein the amine(s) are selected from cyclic secondary amines and the acid(s) are selected from sulfonic acid derivatives, and with the addition of a halogenating agent, wherein S is [CF3S(O)]2O; or CF3S(O)X wherein X means fluoro, chloro, bromo, iodo, a hydroxy group, or an alkaline or alkaline earth metal salt of the hydroxy group; or mixtures thereof.

摘要翻译： 本发明涉及吡唑衍生物亚硫酰化的方法，其特征在于5-氨基-1- [2,6-二氯-4-（三氟甲基）苯基] -1H-吡唑-3-甲腈（II）是 在至少一种胺酸络合物存在下与亚硫酰化剂S反应，其中胺选自环状仲胺，酸选自磺酸衍生物，并且通过加入卤化剂， 其中S是[CF 3 S（O）] 2 O; 或CF 3 S（O）X，其中X表示氟，氯，溴，碘，羟基或羟基的碱金属或碱土金属盐; 或其混合物。