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    Process for preparing N-substituted 1H-pyrazole-5-carbonylchloride compounds
    84.
    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
    85.
    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 manufacturing 5-formyl-pyridine-2,3-dicarboxylic acid esters
    87.
    发明授权
    Process for manufacturing 5-formyl-pyridine-2,3-dicarboxylic acid esters 有权
    5-甲酰基 - 吡啶-2,3-二羧酸酯的制备方法

    公开(公告)号：US08629279B2

    公开(公告)日：2014-01-14

    申请号：US13133013

    申请日：2009-12-07

    申请人： Michael Rack ,  Joachim Gebhardt ,  Frederik Menges ,  Michael Keil ,  Rodney F. Klima ,  David Cortes ,  Robert Leicht ,  Helmut Zech ,  Jochen Schröder

    发明人： Michael Rack ,  Joachim Gebhardt ,  Frederik Menges ,  Michael Keil ,  Rodney F. Klima ,  David Cortes ,  Robert Leicht ,  Helmut Zech ,  Jochen Schröder

    IPC分类号： C07D213/48 ,  C07D213/55

    CPC分类号： C07D213/80

    摘要： A process for manufacturing a 5-formyl-pyridine-2,3-dicarboxylic acid ester (I) wherein Z is hydrogen or halogen; Z1 is hydrogen, halogen, cyano or nitro and R1, R2 are independently C1-C10-alkyl, comprising the steps of (i) reacting a compound of formula (II), wherein the symbols are as in formula (I), with a nitrosation agent (III) R3—O—N═O (III) wherein R3 is C1-C8-alkyl, in the presence of an alkali metal or alkaline earth metal alcoholates or carbonates in a polar aprotic solvent at a temperature of from −45 to 40° C., to obtain an oxime compound (IV) where Z, Z1, R1 and R2 are as in formula (I), and (ii) reacting oxime compound (IV) with an aliphatic C1-C10-aldehyde in the presence of a Lewis acid at a temperature in the range of from 0 to 100° C. The compounds of formula (I) are useful intermediates in the synthesis of herbicidal imidazolinones, like imazamox.

    摘要翻译： 制备其中Z为氢或卤素的5-甲酰基 - 吡啶-2,3-二羧酸酯（I）的方法; Z1是氢，卤素，氰基或硝基，R1，R2独立地是C1-C10-烷基，包括以下步骤：（ⅰ）使符号如式（I）所示的式（ⅱ）化合物与式 在碱金属或碱土金属醇盐或碳酸盐存在下，在极性非质子溶剂中，温度为-45〜40℃的亚硝化剂（Ⅲ）R3-ON = O（Ⅲ）其中R3为C1-C8-烷基 ℃，得到其中Z，Z 1，R 1和R 2如式（I）中的肟化合物（Ⅳ），和（ⅱ）使肟化合物（Ⅳ）与脂族C 1 -C 10 - 醛在 在0至100℃的温度范围内的路易斯酸。式（I）化合物是合成除草咪唑啉酮如咪唑氧化物的有用中间体。

    Process for preparing fluoromethyl-substituted heterocyclic compounds
    90.
    发明授权
    Process for preparing fluoromethyl-substituted heterocyclic compounds 失效
    氟甲基取代的杂环化合物的制备方法

    公开(公告)号：US07994207B2

    公开(公告)日：2011-08-09

    申请号：US12519032

    申请日：2007-12-20

    申请人： Thomas Zierke ,  Michael Rack

    发明人： Thomas Zierke ,  Michael Rack

    IPC分类号： A61K31/415 ,  C07D231/12

    CPC分类号： C07D231/14

    摘要： The present invention relates to a process for preparing fluoromethyl-substituted heterocyclic compounds of the general formula (I) in which R1 is H or F; R2 is an -[A-O]m—R3 group in which A is C2-C4-alkanediyl, R3 is C1-C4-alkyl and m is 1 or 2; by converting the corresponding chloromethyl-substituted compounds (II) in the presence of fluorinating agents, to processes for preparing the chloromethyl-substituted compounds (II), to processes for preparing amides of the general formula (IV) and to compounds of the general formulae (I) and (II).

    摘要翻译： 本发明涉及制备通式（I）的氟甲基取代的杂环化合物的方法，其中R 1为H或F; R2是其中A是C 2 -C 4烷二基，R 3是C 1 -C 4烷基，m是1或2的 - [A-O] m -R 3基团; 通过在氟化剂的存在下将相应的氯甲基取代的化合物（II）转化为制备氯甲基取代的化合物（II）的方法，制备通式（IV）的酰胺的方法和通式 （I）和（II）。