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    Process for the sulfinylation of a pyrazole derivative
    81.
    发明专利
    Process for the sulfinylation of a pyrazole derivative 未知

    公开(公告)号：AU2007316721A1

    公开(公告)日：2008-05-15

    申请号：AU2007316721

    申请日：2007-11-05

    Applicant: BASF SE

    Inventor： GRONING CARSTEN ,  SUKOPP MARTIN ,  KUHN OLIVER ,  KEIL MICHAEL ,  LONGLET JON J

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

    Abstract: 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.

    Process for the sulfinylation of a pyrazole derivative
    82.
    发明专利
    Process for the sulfinylation of a pyrazole derivative 未知

    公开(公告)号：AU2007316718A1

    公开(公告)日：2008-05-15

    申请号：AU2007316718

    申请日：2007-11-05

    Applicant: BASF SE

    Inventor： KUHN OLIVER ,  LONGLET JON J ,  SUKOPP MARTIN ,  KEIL MICHAEL ,  GRONING CARSTEN

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

    Abstract: The present invention relates to a process for the 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 DIFLUOROMETHYLPYRAZOLYL CARBOXYLATES
    83.
    发明专利
    PROCESS FOR PREPARING DIFLUOROMETHYLPYRAZOLYL CARBOXYLATES 未知

    公开(公告)号：CA2666746A1

    公开(公告)日：2008-05-08

    申请号：CA2666746

    申请日：2007-11-02

    Applicant: BASF SE

    Inventor： DIETZ JOCHEN ,  KEIL MICHAEL ,  LOHMANN JAN KLAAS ,  ZIERKE THOMAS ,  SMIDT SEBASTIAN PEER ,  RACK MICHAEL ,  GROTE THOMAS ,  RHEINHEIMER JOACHIM ,  SUKOPP MARTIN ,  LOEHR SANDRA

    IPC: C07D237/04 ,  C07F7/04

    Abstract: The present invention relates to a process for preparing difluoromethyl-s ubstituted 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 formul a (II) in which X is fluorine, chlorine, or bromine, R1 has one of the defin itions 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 R 3 nSiCl(4-n) in which n is 1, 2 or 3 and the substituents R3 are each indepe ndently selected from C1-C8-alkyl and phenyl, and with a metal which is sele cted from the metals of groups 1, 2, 3, 4 and 12 of the periodic table and h as a redox potential of less than -0.7 V, based on a standard hydrogen elect rode (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.

    METODO PARA LA PRODUCCION DE 3-FENIL(TIO)URACILOS Y 3-FENILDITIOURACILOS.
    86.
    发明专利
    METODO PARA LA PRODUCCION DE 3-FENIL(TIO)URACILOS Y 3-FENILDITIOURACILOS. 未知

    公开(公告)号：ES2295957T3

    公开(公告)日：2008-04-16

    申请号：ES04803387

    申请日：2004-12-01

    Applicant: BASF SE

    Inventor： HAMPRECHT GERHARD ,  PUHL MICHAEL ,  WOLF BERND ,  KEIL MICHAEL ,  REINHARD ROBERT ,  SEITZ WERNER

    IPC: C07D239/56 ,  C07D239/54

    Abstract: Proceso para preparar 3-fenil(tio)uracilo o 3-fenilditiouracilo de la fórmula I En la cual las variables tienen los siguientes significados: R1 es hidrógeno, ciano, amino, alquilo de C1-C6, cianoalquilo de C1-C3, haloalquilo de C1-C6, haloalcoxi de C1-C6, cicloalquil de C3-C7, C2-C6-alquenilo, haloalquenilo de C2-C6, alquinilo de C3-C6, haloalquinilo de C3-C6 o fenil- alquilo de C1-C4; R2 y R3 son, independientemente uno de otro, hidrógeno, alquilo de C1- C6, haloalquilo de C1-C6, cicloalquilo de C3-C7, alquenilo de C2-C6, haloalquenilo de C2-C6, alquinilo de C3-C6 o haloalquinilo de C3-C6; X1, X2 y X3 son, independientemente unos de otros, oxígeno o azufre; Ar es fenilo que puede sustituirse uno o varias veces por los siguientes grupos: hidrógeno, halógeno, ciano, alquilo de C1-C4 o haloalquilo de C1-C4; y A es un radical derivado de una amina primaria o secundaria o NH2; el cual comprende la reacción de un feniliso(tio)cianato de la fórmula II en la cual las variables X1, X3, Ar y A tienen los significados ya mencionados, con una enamina de la fórmula III en la cual R1a tiene los significados ya mencionados para R1 con la excepción de amino; R2, R3 y X2 tienen los significados ya mencionados; y R4 representa alquilo de C1-C6, haloalquilo de C1-C6, alcoxi de C1-C3- alquilo de C1-C3, alquiltio de C1-C3- alquilo de C1-C3, alquenilo de C2-C6, haloalquenilo de C2-C6, alquinilo de C3-C6, haloalquinilo de C3-C6, cicloalquilo de C3-C7, cianoalquilo de C1-C6 o bencilo, que por su parte no está sustituido o sustituido en el anillo de fenilo por metilo, metoxi, metiltio, halógeno, nitro o ciano; en presencia de 1, 8 hasta 2, 6 equivalentes de base por mol de feniliso(tio)-cianato de la fórmula II; y opcionalmente en otro paso la reacción del 3-fenil(tio)uracilo o 3-fenilditiouracilo resultante de la fórmula I cuando R1=R1a, si R1 representa hidrógeno, con un agente de aminación de la fórmula IV H2N-L1 IV, en la cual L1 representa un grupo saliente desplazable nucleofilo, para producir3-fenil(tio)uracilo o 3-fenilditiouracilo de la fórmula I cuando R1=Amino.

    METHOD FOR PRODUCING SUBSTITUTED BIPHENYLS
    88.
    发明专利
    METHOD FOR PRODUCING SUBSTITUTED BIPHENYLS 未知

    公开(公告)号：CA2727075C

    公开(公告)日：2016-05-31

    申请号：CA2727075

    申请日：2009-06-22

    Applicant: BASF SE

    Inventor： MAYWALD VOLKER ,  SMIDT SEBASTIAN PEER ,  WISSEL-STOLL KATHRIN ,  SCHMIDT-LEITHOFF JOACHIM ,  ALTENHOFF ANSGAR GEREON ,  KEIL MICHAEL

    IPC: C07C205/11 ,  C07C205/12

    Abstract: The invention relates to a method for producing substituted biphenyls of formula (I), wherein R1 = nitro or amino, R2 = cyano, halide, C1-C4 alkyl halide, C1-C4 alkoxy halide or C1-C4 alkylthio halide, n = 0 to 3 and R3 = hydrogen, cyano or halide, characterized by reacting a halobenzene of formula (I1), wherein HaI represents chlorine or bromine, with a phenyl boronic acid (IVa) of a diphenyl borinic acid (IVb) or a mixture of (IVa) and (IVb) in a solvent or diluent in the presence of a base and of a palladium catalyst which consists of palladium and a bidentate phosphorus ligand of formula (III), wherein Ar represents optionally substituted phenyl and R4 and R5 represent C1-C8 alkyl or C3-C6 cycloalkyl each or together form a two- to seven-membered bridge which can optionally carry a C1-C6 alkyl substituent.

    METHOD FOR MANUFACTURING ARYL CARBOXAMIDES
    90.
    发明专利
    METHOD FOR MANUFACTURING ARYL CARBOXAMIDES 未知

    公开(公告)号：CA2721695C

    公开(公告)日：2016-04-12

    申请号：CA2721695

    申请日：2009-05-06

    Applicant: BASF SE

    Inventor： REICHERT WOLFGANG ,  KORADIN CHRISTOPHER ,  SMIDT SEBASTIAN PEER ,  MAYWALD VOLKER ,  WOLF BERND ,  RACK MICHAEL ,  ZIERKE THOMAS ,  KEIL MICHAEL

    IPC: C07D213/82 ,  C07C231/02 ,  C07C233/57 ,  C07C233/64 ,  C07D231/14 ,  C07D231/16

    Abstract: Method for manufacturing aryl carboxamides of the formula (I), with Ar = singly to triply substituted phenyl , pyridyl or pyrazolyl rings, wherein the substituents are selected from halogen, C1-C4 alkyl and C1-C4 halogen alkyl; M = thienyl or phenyl, which can contain a halogen substituent; Q = direct bond, cyclopropylene, annulated bicyclo [2.2.1]heptane or bicyclo[2.2.1]heptene ring; R1 = hydrogen, halogen, C1-C6 alkyl, C1-C4 alkoxy, C1-C4 halogen alkoxy, singly to triply substituted phenyl, wherein the substituents are selected from halogen and trifluoromethylthio, or cyclopropyl; through reaction of an acid chloride of the formula (II) with an aryl amine (III) in a suitable non-aqueous solvent, wherein in the absence of an auxiliary base a) the acid chloride (II) is added, b) a pressure of 0 to 700 mbar is established, c) the aryl amine (III) is added in approximately stoichiometric amounts and d) the valuable product is isolated.

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