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    Method for the production of benzophenonen
    1.
    发明申请
    Method for the production of benzophenonen 有权
    二苯甲酮生产方法

    公开(公告)号：US20060009659A1

    公开(公告)日：2006-01-12

    申请号：US10535710

    申请日：2003-12-01

    申请人： Volker Maywald ,  Nico Hoffmann ,  Michael Keil ,  Uwe Vogelbacher ,  Jan Wevers

    发明人： Volker Maywald ,  Nico Hoffmann ,  Michael Keil ,  Uwe Vogelbacher ,  Jan Wevers

    IPC分类号： C07C45/46

    CPC分类号： C07C51/363 ,  C07C45/46 ,  C07C45/81 ,  C07C51/60 ,  C07C49/84 ,  C07C65/21

    摘要： A process for preparing benzophenones of the formula I, where X may be chlorine, hydroxyl, methoxy or C1-C6-alkylcarbonyloxy, and Y may be chlorine or bromine, by reacting an acid chloride of the formula II where X and Y are as defined above with 3,4,5-trimethoxytoluene, which comprises carrying out the reaction in the presence of a) an aromatic hydrocarbon as a diluent and b) from 0.01 to 0.2 mol % of an iron catalyst, based on the acid chloride, c) at a temperature between 60° C. and the boiling point of the particular diluent.

    摘要翻译： 制备式I的二苯甲酮的方法，其中X可以是氯，羟基，甲氧基或C 1 -C 6 - 烷基羰氧基，Y可以是氯或溴， 通过使式II的酰氯与其中X和Y如上所定义的酰氯与3,4,5-三甲氧基甲苯反应，其包括在a）芳族烃作为稀释剂存在下进行反应，和b）从0.01至 0.2mol％的铁催化剂，基于酰氯，c）在60℃和特定稀释剂的沸点之间的温度下。

    Method for the production of benzophenones
    2.
    发明授权
    Method for the production of benzophenones 有权
    二苯甲酮生产方法

    公开(公告)号：US07253323B2

    公开(公告)日：2007-08-07

    申请号：US10535710

    申请日：2003-12-01

    申请人： Volker Maywald ,  Nico Hoffmann ,  Michael Keil ,  Uwe Josef Vogelbacher ,  Jan Hendrik Wevers

    发明人： Volker Maywald ,  Nico Hoffmann ,  Michael Keil ,  Uwe Josef Vogelbacher ,  Jan Hendrik Wevers

    IPC分类号： C07C45/00

    CPC分类号： C07C51/363 ,  C07C45/46 ,  C07C45/81 ,  C07C51/60 ,  C07C49/84 ,  C07C65/21

    摘要： A process for preparing benzophenones of the formula I, where X may be chlorine, hydroxyl, methoxy or C1-C6-alkylcarbonyloxy, and Y may be chlorine or bromine, by reacting an acid chloride of the formula II where X and Y are as defined above with 3,4,5-trimethoxytoluene, which comprises carrying out the reaction in the presence of a) an aromatic hydrocarbon as a diluent and b) from 0.01 to 0.2 mol % of an iron catalyst, based on the acid chloride, c) at a temperature between 60° C. and the boiling point of the particular diluent.

    摘要翻译： 制备式I的二苯甲酮的方法，其中X可以是氯，羟基，甲氧基或C 1 -C 6 - 烷基羰氧基，Y可以是氯或溴， 通过使式II的酰氯与其中X和Y如上所定义的酰氯与3,4,5-三甲氧基甲苯反应，其包括在a）芳族烃作为稀释剂存在下进行反应，和b）从0.01至 0.2mol％的铁催化剂，基于酰氯，c）在60℃和特定稀释剂的沸点之间的温度下。

    Method for preparing 1,3,4-substituted pyrazol compounds
    4.
    发明授权
    Method for preparing 1,3,4-substituted pyrazol compounds 有权
    制备1,3,4-取代吡唑化合物的方法

    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。

    Method for manufacturing aryl carboxamides
    5.
    发明授权
    Method for manufacturing aryl carboxamides 有权
    芳基甲酰胺的制备方法

    公开(公告)号：US08350046B2

    公开(公告)日：2013-01-08

    申请号：US12990892

    申请日：2009-05-06

    申请人： Wolfgang Reichert ,  Christopher Koradin ,  Sebastian Peer Smidt ,  Volker Maywald ,  Bernd Wolf ,  Michael Rack ,  Thomas Zierke ,  Michael Keil

    发明人： Wolfgang Reichert ,  Christopher Koradin ,  Sebastian Peer Smidt ,  Volker Maywald ,  Bernd Wolf ,  Michael Rack ,  Thomas Zierke ,  Michael Keil

    IPC分类号： C07D213/82 ,  C07D231/14

    CPC分类号： C07C231/02 ,  C07C2601/14 ,  C07D213/82 ,  C07D231/14 ,  C07D231/16 ,  C07C233/65 ,  C07C233/75

    摘要： A process for preparing arylcarboxamides of the formula (I) where Ar=a mono- to trisubstituted phenyl, pyridyl or pyrazolyl ring, where the substituents are selected from halogen, C1-C4-alkyl and C1-C4-haloalkyl; M=thienyl or phenyl, which may bear a halogen substituent; Q=direct bond, cyclopropylene, fused bicyclo[2.2.1]heptane or bicyclo[2.2.1]heptene ring; R1=hydrogen, halogen, C1-C6-alkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, mono- to trisubstituted phenyl, where the substituents are selected from halogen and trifluoromethylthio, or cyclopropyl; by reacting an acid chloride of the formula (II) with an arylamine (III) in a suitable nonaqueous solvent, wherein, in the absence of an auxiliary base, a) the acid chloride (II) is initially charged, b) a pressure of from 0 to 700 mbar is established, c) the arylamine (III) is metered in an approximately stoichiometric amount and d) the product of value is isolated.

    摘要翻译： 制备式（I）的芳基羧酰胺的方法，其中Ar =单 - 三取代的苯基，吡啶基或吡唑基环，其中取代基选自卤素，C 1 -C 4 - 烷基和C 1 -C 4卤代烷基; M =噻吩基或苯基，其可以带有卤素取代基; Q =直接键合，亚环丙基，稠合双环[2.2.1]庚烷或双环[2.2.1]庚烯环; R1 =氢，卤素，C1-C6-烷基，C1-C4-烷氧基，C1-C4-卤代烷氧基，一至三取代的苯基，其中取代基选自卤素和三氟甲硫基，或环丙基; 通过使式（II）的酰氯与芳基胺（III）在合适的非水溶剂中反应，其中在没有辅助碱的情况下，a）最初加入酰氯（II），b） 建立0至700毫巴，c）芳基胺（III）以约化学计量的量计量，并且d）分离产物的值。

    Process for preparing alkyl 2-alkoxymethylene-4,4-difluoro-3-oxobutyrates
    9.
    发明申请
    Process for preparing alkyl 2-alkoxymethylene-4,4-difluoro-3-oxobutyrates 有权
    制备2-烷氧基亚甲基-4,4-二氟-3-氧代丁酸烷基酯的方法

    公开(公告)号：US20110004002A1

    公开(公告)日：2011-01-06

    申请号：US12919842

    申请日：2009-02-27

    申请人： Volker Maywald ,  Sebastian Peer Smidt ,  Bernd Wolf ,  Christopher Koradin ,  Thomas Zierke ,  Michael Rack ,  Michael Keil

    发明人： Volker Maywald ,  Sebastian Peer Smidt ,  Bernd Wolf ,  Christopher Koradin ,  Thomas Zierke ,  Michael Rack ,  Michael Keil

    IPC分类号： C07D231/14 ,  C07C69/66

    CPC分类号： C07D231/14 ,  C07C67/343 ,  C07C69/72

    摘要： A process for preparing alkyl 2-alkoxymethylene-4,4-difluoro-3-oxobutyrates (VI) where R is methyl or ethyl, from crude reaction mixtures of alkyl 4,4-difluoroacetoacetates (I) by a) reacting where M is a sodium or potassium ion, and without additional solvent to form an enolate (V) b) releasing the corresponding alkyl 4,4-difluoroacetoacetate (I) from the enolate (V) by means of acid, c) removing the salt formed from cation M and acid anion as a solid and d) converting (I), without isolation from the crude reaction mixture, to the alkyl 2-alkoxymethylene-4,4-difluoro-3-oxobutyrate (VI), and the use of (VI) for preparing 1-methyl-3-difluoromethyl-pyrazol-3-ylcarboxyates VII

    摘要翻译： 由烷基4,4-二氟乙酰乙酸酯（I）的粗反应混合物制备R为甲基或乙基的2-烷氧基亚甲基-4,4-二氟-3-氧代丁酸烷基酯（VI）的方法，通过a）使M 钠离子或钾离子，无另外的溶剂以形成烯醇化物（Ⅴ）b）通过酸从烯醇化物（Ⅴ）中释出相应的4,4-二氟乙酰乙酸烷基酯（Ⅰ），c）除去由阳离子M形成的盐 和酸阴离子作为固体，以及d）将（I）从粗反应混合物中分离出来，转化为2-烷氧基亚甲基-4,4-二氟-3-氧代丁酸烷基酯（VI），以及（VI）用于 制备1-甲基-3-二氟甲基 - 吡唑-3-基羧酸酯VII

    Method for production of aryl-substituted annelated pyrimidines
    10.
    发明申请
    Method for production of aryl-substituted annelated pyrimidines 审中-公开
    芳基取代的环状嘧啶的制备方法

    公开(公告)号：US20100087640A1

    公开(公告)日：2010-04-08

    申请号：US12521877

    申请日：2008-01-10

    申请人： Bernd Wolf ,  Volker Maywald ,  Michael Keil ,  Manuel Budich ,  Michael Rack ,  Manfred Ehresmann

    发明人： Bernd Wolf ,  Volker Maywald ,  Michael Keil ,  Manuel Budich ,  Michael Rack ,  Manfred Ehresmann

    IPC分类号： C07D487/04

    CPC分类号： C07D487/04

    摘要： The present invention relates to a process for preparing aryl-substituted fused pyrimidines of the general formula (I) in which L1 to L5 are H, halogen, CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy etc.; Y1 to Y3 are C—RY or N; RY is H or optionally substituted C1-C4-alkyl or two adjacent RY together form a ring; X is OH, Cl or Br; which comprises (i) the reaction of a 2-phenylmalonate with a compound (III) or a tautomer thereof, in the presence of a suitable base, where the alcohol, released during the reaction, of the formula R—OH is continuously removed from the reaction mixture under reduced pressure; giving a compound of the formula (I) or a salt thereof in which X is OH, and, if X in the compounds of the general formula (I) is chlorine or bromine, (ii) the reaction of the compounds of the formula (I) obtained in step (i) or the salts with a halogenating agent.

    摘要翻译： 本发明涉及制备通式（I）的芳基取代的稠合嘧啶的方法，其中L 1至L 5为H，卤素，CN，NO 2，C 1 -C 4烷基，C 1 -C 4卤代烷基，C 1 -C 4 - 烷氧基，C1-C4-卤代烷氧基等; Y1至Y3为C-RY或N; RY为H或任选取代的C 1 -C 4烷基或两个相邻的RY一起形成环; X是OH，Cl或Br; 其包括（i）2-苯基丙二酸酯与化合物（III）或其互变异构体在合适的碱的存在下反应，其中反应期间释放的醇与式R-OH的连续从 减压下的反应混合物; 得到其中X是OH的式（I）化合物或其盐，并且如果通式（I）的化合物中的X是氯或溴，则（ii）式（I）化合物 I）或与卤化剂的盐。