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    Process for manufacturing substituted 3-pyridylmethyl ammonium bromides
    44.
    发明公开
    Process for manufacturing substituted 3-pyridylmethyl ammonium bromides 审中-公开
    制备取代的3-吡啶基甲基溴化铵的方法

    公开(公告)号：EP2365965A1

    公开(公告)日：2011-09-21

    申请号：EP09755886.0

    申请日：2009-11-13

    申请人： BASF SE

    发明人： GEBHARDT, Joachim ,  MENGES, Frederik ,  RACK, Michael ,  KEIL, Michael ,  SCHRÖDER, Jochen ,  ORSTEN, Stefan ,  ZECH, Helmut ,  KLIMA, Rodney, F. ,  CORTES, David ,  LEICHT, Robert ,  YEGERLEHNER, Tony

    IPC分类号： C07D213/80 ,  C07D401/04 ,  A61K31/44 ,  A61K31/4439

    CPC分类号： C07D401/04 ,  C07D213/80 ,  C07D401/06 ,  C07D403/06 ,  C07D413/06 ,  C07D417/06

    摘要： A process for manufacturing 5,6-disubstituted-3-pyridylmethyl ammonium bromides (I), wherein Q is a tertiary aliphatic or cyclic, saturated, partially unsaturated or aromatic amine; Z is hydrogen or halogen; Z1 is hydrogen, halogen, cyano or nitro; Y and Y1 are each independently OR1, NR1R2, or when taken together YY1 is —O—, —S— or NR3—; R1 and R2 are each independently hydrogen, C1-C4 alkyl optionally substituted with C1-C4 alkoxy or phenyl optionally substituted with one to three C1-C4 alkyl groups, C1-C4 alkoxy groups or halogen atoms, or phenyl optionally substituted with one to three C1-C4 alkyl groups, C1-C4 alkoxy groups or halogen atoms; R3 is hydrogen or C1-C4 alkyl; comprises the steps of (i) reacting a compound of formula (II), wherein the symbols have the meaning given in formula (I), with bromine in the presence of a radical initiator in a solvent mixture comprising an aqueous phase and an organic phase, where the organic phase comprises a solvent selected from 1,2-dichloroethane, chlorobenzene, 1,2-dichlorobenzene, 1,3-dichlorobenzene, 1,4-dichlorobenzene and tetrachloromethane, and where the pH-value of the aqueous phase is from 3 to

    摘要翻译： 制备5,6-二取代-3-吡啶基甲基溴化铵（I）的方法包括以下步骤：（i）使式（II）化合物反应，得到3-溴甲基-5,6-二取代的吡啶化合物（ （ii）使式（III）的溴化合物与叔胺碱Q在溶剂中在约0℃至100℃的温度范围内反应。

    PROCESS FOR PREPARING ALKYL 2-ALKOXYMETHYLENE-4,4-DIFLUORO-3-OXOBUTYRATES
    45.
    发明公开
    PROCESS FOR PREPARING ALKYL 2-ALKOXYMETHYLENE-4,4-DIFLUORO-3-OXOBUTYRATES 有权
    用于生产2-烷氧基亚甲基-4,4-二氟-3-OXOBUTTERSÄUREALKYLESTERN

    公开(公告)号：EP2262756A1

    公开(公告)日：2010-12-22

    申请号：EP09715410.8

    申请日：2009-02-27

    申请人： BASF SE

    发明人： MAYWALD, Volker ,  SMIDT, Sebastian, Peer ,  WOLF, Bernd ,  KORADIN, Christopher ,  ZIERKE, Thomas ,  RACK, Michael ,  KEIL, Michael

    IPC分类号： C07C67/343 ,  C07C69/72

    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 alkyl acetate (II), RO M alkoxide (III), where M is a sodium or potassium ion, and alkyl difluoroacetate (IV), 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).

    VERFAHREN ZUR HERSTELUNG VON SULFONSÄUREDIAMIDEN
    46.
    发明公开
    VERFAHREN ZUR HERSTELUNG VON SULFONSÄUREDIAMIDEN 审中-公开
    VERFAHREN ZUR HERSTELUNG VONSULFONSÄUREDIAMIDEN

    公开(公告)号：EP2200978A1

    公开(公告)日：2010-06-30

    申请号：EP08838788.1

    申请日：2008-10-10

    申请人： BASF SE

    发明人： PLESCHKE, Axel ,  SCHMIDT, Thomas ,  GEBHARDT, Joachim ,  LÖHR, Sandra ,  KEIL, Michael ,  WEVERS, Jan Hendrik

    IPC分类号： C07C303/34 ,  C07C307/06 ,  C07D239/54

    CPC分类号： C07C303/34 ,  A01N43/54 ,  C07C307/06 ,  C07C381/00 ,  C07D239/54

    摘要： The present invention relates to a method for producing sulfonic acid amines of the general formula (I) R1R2N-S(O)2-NH2 (I), where R1 and R2 are independent of each other and stand for a primary alkyl radical having 1 to 8 C atoms, a secondary alkyl radical having 3 to 8 C atoms, or a cycloalkyl radical having 5 to 8 C atoms, or, together with the nitrogen atom, form a 5- to 8-member saturated nitrogen heterocyclic compound that can comprise, in addition to the nitrogen atom, an additional hetero atom, selected from O and S, as a ring member, wherein the nitrogen heterocyclic compound is unsubstituted, or can comprise 1, 2, 3, or 4 alkyl groups each having 1 to 4 C atoms as substituents. The method comprises the following steps: i) conversion of a secondary amine of the formula (II) R1R2NH (II), where R1 and R2 have the meaning indicated above, having sulfuryl chloride in an inert, particularly aromatic, solvent in the presence of a tertiary amine, to form a sulfamoyl chloride of the formula (III) R1R2N-S(O)2-CI (III), where R1 and R2 have the meaning indicated above, and ii) conversion of the sulfamoyl chloride of the formula (III) obtained in step i) using ammonia, wherein in step ii) the sulfamoyl chloride of the formula (III) is used in the form of the solution obtained in step i) in the inert, particularly aromatic, solvent.

    摘要翻译： 本发明涉及通式（I）R 1 R 2 N-S（O）2 -NH 2（I）的磺酸胺的制备方法，其中R 1和R 2彼此独立并且代表具有1 具有3至8个C原子的仲烷基或具有5至8个C原子的环烷基，或者与该氮原子一起形成5至8元饱和氮杂环化合物，该化合物可包含 除了氮原子之外，还可以包含选自O和S的另外的杂原子作为环成员，其中氮杂环化合物是未取代的，或者可以包含1,2,3或4个各自具有1至4个 C原子作为取代基。 该方法包括以下步骤：i）将式（II）的仲胺在惰性溶剂，特别是芳香溶剂存在下转化其中R1和R2具有上述含义的式IIR2NH（II） 形成式（III）R 1 R 2 N-S（O）2 -Cl（III）的氨磺酰氯，其中R 1和R 2具有上述含义，和ii）将式 其中在步骤ii）中，式（III）的氨磺酰氯以在步骤i）中获得的溶液形式在惰性溶剂，特别是芳香溶剂中使用。

    VERFAHREN ZUR HERSTELLUNG VON DIFLUORMETHYLPYRAZOLYLCARBOXYLATEN
    48.
    发明授权
    VERFAHREN ZUR HERSTELLUNG VON DIFLUORMETHYLPYRAZOLYLCARBOXYLATEN 有权
    用于生产DIFLUORMETHYLPYRAZOLYLCARBOXYLATEN

    公开(公告)号：EP2086944B1

    公开(公告)日：2010-01-13

    申请号：EP07822162.9

    申请日：2007-11-02

    申请人： BASF SE

    发明人： RACK, Michael ,  SMIDT, Sebastian Peer ,  LÖHR, Sandra ,  KEIL, Michael ,  DIETZ, Jochen ,  RHEINHEIMER, Joachim ,  GROTE, Thomas ,  ZIERKE, Thomas ,  LOHMANN, Jan Klaas ,  SUKOPP, Martin

    IPC分类号： C07D237/04 ,  C07F7/04

    CPC分类号： C07D231/14

    摘要： The present invention relates to a process for preparing difluoromethyl-substituted pyrazol-4-yl carboxylates 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 definitions 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 each independently selected from C1-C8-alkyl and phenyl, and with a metal which is selected from the metals of groups 1, 2, 3, 4 and 12 of the periodic table and has a redox potential of less than -0.7 V, based on a standard 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) in which R2 has one of the definitions given above.

    PROCESS FOR THE SULFINYLATION OF A PYRAZOLE DERIVATIVE
    49.
    发明公开
    PROCESS FOR THE SULFINYLATION OF A PYRAZOLE DERIVATIVE 有权
    方法亚磺酰化的吡唑衍生物

    公开(公告)号：EP2081908A1

    公开(公告)日：2009-07-29

    申请号：EP07822220.5

    申请日：2007-11-05

    申请人： BASF SE

    发明人： SUKOPP, Martin ,  KUHN, Oliver ,  GRÖNING, Carsten ,  KEIL, Michael ,  LONGLET, Jon J.

    IPC分类号： C07D231/44 ,  A01N43/56 ,  A01N43/00 ,  A61K31/415 ,  A61P33/00

    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.

    PROCESS FOR PREPARING SUBSTITUTED BIPHENYLS
    50.
    发明公开
    PROCESS FOR PREPARING SUBSTITUTED BIPHENYLS 审中-公开
    程序就取代的联苯类的制备

    公开(公告)号：EP2029519A1

    公开(公告)日：2009-03-04

    申请号：EP07729695.2

    申请日：2007-05-31

    申请人： BASF SE

    发明人： SMIDT, Sebastian, Peer ,  DIETZ, Jochen ,  KEIL, Michael ,  GROTE, Thomas

    IPC分类号： C07C201/12 ,  C07C209/68 ,  C07C205/12 ,  C07C211/52

    CPC分类号： C07C201/12 ,  C07C209/68 ,  C07C211/52 ,  C07C205/12

    摘要： A process for preparing substituted biphenyls of the formula (I), in which the substituents are defined as follows: X is fluorine or chlorine; R1 is nitro, amino or NHR3; R2 is cyano, nitro, halogen, C1-C6-alkyl, C1-C6-alkenyl, C1-C6-alkynyl, C1-C6-alkoxy, C1-C6-haloalkyl, C1-C6-alkylcarbonyl or phenyl; R3 is C1-C4-alkyl, C1-C4-alkenyl or C1-C4-alkynyl; n is 1, 2 or 3, where in case that n is 2 or 3, the R2 radicals may also be different, which comprises reacting the compound of the formula (II), in which Hal is halogen and X and R1 are as defined above, in the presence of a base and of a palladium catalyst selected from the group of: a) palladium-triarylphosphine or -trialkylphosphine complex with palladium in the zero oxidation state, b) salt of palladium in the presence of triarylphospine or trialkylphosphine as a complex ligand or c) metallic palladium, optionally applied to support, in the presence of triarylphosphine or trialkylphosphine, in a solvent, with a diphenylborinic acid (III), in which R2 and n are as defined above, where the triarylphosphines or trialkylphosphines used may be substituted.