公开(公告)号：EP2782910A1

公开(公告)日：2014-10-01

申请号：EP12794238.1

申请日：2012-11-20

Applicant: BASF SE

Inventor： DOCHNAHL, Maximilian ,  KÖRBER, Karsten ,  DESHMUKH, Prashant ,  KAISER, Florian ,  RACK, Michael ,  FRASSETTO, Timo ,  VEITCH, Gemma

IPC: C07D401/04 ,  C07D471/10

CPC classification number: C07D401/04 ,  C07D471/10

Abstract: The present invention relates to a process for preparing an N-substituted 1 H-pyrazole- 5- carboxylate compound of the formula (l-A) comprising the steps of i) deprotonating a compound of the formula (II) in which the variables R
1 , R
2 and r are each as defined in the description and the claims, with a magnesium-organic base having a carbon bound magnesium; and ii) subjecting the product obtained in step (i) to a carbonylation by reacting it with a reagent selected from the group consisting carbon dioxide or a carbon dioxide equivalent, to obtain a compound of formula (l-A); and it relates to further conversions to yield a N-substituted 1H-pyrazole-5-carbonyl chloride compound of the formula (I).

公开(公告)号：EP2132167B1

公开(公告)日：2013-12-25

申请号：EP08717291.2

申请日：2008-02-29

Applicant: BASF SE

Inventor： VOGELBACHER, Uwe Josef ,  OTTO, Peter ,  RACK, Michael

IPC: C07C253/30 ,  C07D487/04

CPC classification number: C07D487/04 ,  C07C253/30 ,  C07C2601/08 ,  C07C2601/14 ,  C07C255/17 ,  C07C255/40

Abstract: The present invention relates to a process for preparing beta-ketonitriles of the general formula I in which R1 is, inter alia, C1-C12-alkyl, C2-C12-alkenyl, C2-C12-alkinyl, C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C4-alkyl, phenyl-C1-C4-alkyl, phenoxy-C1-C4-alkyl or benzyloxy-C1-C4-alkyl; R2 is, inter alia, hydrogen, C1-C12-alkyl, C2-C12-alkenyl, C2-C12-alkinyl, C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C4-alkyl, phenyl, phenyl-C1-C4-alkyl, phenoxy-C1-C4-alkyl or benzyloxy-C1-C4-alkyl, which comprises reacting a nitrile of the formula II in which R1 has one of the meanings given above with a carboxylic ester of the formula III in which R2 has one of the meanings given above and R3 is C1-C12-alkyl, C1-C4-alkoxy-C1-C4-alkyl, C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C4-alkyl, phenyl-C1-C4-alkyl, phenoxy-C1-C4-alkyl or benzyloxy-C1-C4-alkyl, where the reaction is carried out in the presence of a potassium alkoxide and at least 80% of the nitrile of the formula II are added to the reaction under reaction conditions.

Abstract translation: 本发明涉及一种制备通式Ⅰ的α-溴代腈的方法，其中R 1特别是C 1 -C 12 - 烷基，C 2 -C 12 - 烯基，C 2 -C 12 - 炔基，C 3 -C 8 - 环烷基， C 3 -C 8 - 环烷基-C 1 -C 4 - 烷基，苯基-C 1 -C 4 - 烷基，苯氧基-C 1 -C 4烷基或苄氧基-C 1 -C 4烷基; R2特别是氢，C 1 -C 12 - 烷基，C 2 -C 12 - 烯基，C 2 -C 12 - 炔基，C 3 -C 8 - 环烷基，C 3 -C 8 - 环烷基-C 1 -C 4 - 烷基，苯基， C 4 - 烷基，苯氧基-C 1 -C 4 - 烷基或苄氧基-C 1 -C 4 - 烷基，其包括使其中R 1具有上述含义之一的式II的腈与式III的羧酸酯反应，其中R 2 具有上述含义之一，R 3为C 1 -C 12 - 烷基，C 1 -C 4 - 烷氧基-C 1 -C 4 - 烷基，C 3 -C 8 - 环烷基，C 3 -C 8 - 环烷基-C 1 -C 4烷基，苯基-C C 4 - 烷基，苯氧基-C 1 -C 4 - 烷基或苄氧基-C 1 -C 4烷基，其中反应在醇盐存在下进行，并且将至少80％的式II的腈加入到反应中 在反应条件下。

公开(公告)号：EP2370410B1

公开(公告)日：2013-10-23

申请号：EP09745045.6

申请日：2009-11-03

Applicant: BASF SE

Inventor： MENGES, Frederik ,  GEBHARDT, Joachim ,  RACK, Michael ,  KEIL, Michael ,  KLIMA, Rodney F. ,  CORTES, David ,  LEICHT, Robert ,  ZECH, Helmut ,  SCHRÖDER, Jochen

IPC: C07D213/81 ,  C07D401/04

CPC classification number: C07D401/04 ,  C07D213/81

公开(公告)号：EP2315760B1

公开(公告)日：2013-03-06

申请号：EP09780999.0

申请日：2009-07-23

Applicant: BASF SE

Inventor： PARRA RAPADO, Liliana ,  HUPE, Eike ,  WITSCHEL, Matthias ,  SEITZ, Thomas ,  SIMON, Anja ,  REINHARD, Robert ,  SIEVERNICH, Bernd ,  GROßMANN, Klaus ,  EHRHARDT, Thomas ,  NEWTON, Trevor William ,  STELZER, Frank ,  QU, Tao ,  MOBERG, William Karl ,  SONG, Dschun ,  RACK, Michael ,  FRASSETTO, Timo ,  KREUZ, Klaus ,  MAJOR, Julia

IPC: C07D401/06 ,  C07D403/06 ,  A01N43/60

CPC classification number: C07D401/06 ,  A01N43/60 ,  A01N43/78 ,  A01N43/80 ,  A01N43/82 ,  A01N43/84 ,  A01N43/90 ,  C07D403/06 ,  A01N33/18 ,  A01N43/54 ,  A01N2300/00

公开(公告)号：EP2349987B1

公开(公告)日：2012-11-14

申请号：EP09783451.9

申请日：2009-09-28

Applicant: BASF SE ,  Merial Limited

Inventor： SUKOPP, Martin ,  KORTE, Alexander ,  FÜLSTER, Stefan ,  KEIL, Michael ,  RACK, Michael

IPC: C07C303/42 ,  C07D231/44 ,  C07C313/02 ,  C07C313/04 ,  A01N43/00

CPC classification number: C07D231/44 ,  C07C313/04

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

Applicant: BASF SE

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

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

CPC classification number: C07D401/04 ,  C07D213/80 ,  C07D401/06 ,  C07D403/06 ,  C07D413/06 ,  C07D417/06

Abstract: 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

Abstract translation: 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。

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

Applicant: BASF SE

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

IPC: C07C67/343 ,  C07C69/72

CPC classification number: C07D231/14 ,  C07C67/343 ,  C07C69/72

Abstract: 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).

公开(公告)号：EP1127050B1

公开(公告)日：2010-08-25

申请号：EP99955919.8

申请日：1999-10-30

Applicant: BASF SE

Inventor： GÖTZ, Norbert ,  GÖTZ, Roland ,  RACK, Michael

IPC: C07D231/18 ,  C07C243/30 ,  C07C241/04

CPC classification number: C07C243/30 ,  C07D231/20

Abstract: The invention relates to a method for producing substituted hydroxypyrazoles and new intermediate products. It relates in particular to a method for producing compounds of formula (I) in which R1 is hydrogen, an aliphatic group with between 1 and 8 carbon atoms, C¿1?-C6-alkoxycarbonyl, C1-C6-alkyl thiocarbonyl or a cyclic ring system with between 3 and 14 ring atoms; R?2¿ is hydrogen, an aliphatic group with between 1 and 8 carbon atoms; or R?1 and R2¿ together with the carbon atom to which they are bound are a cyclic or bicyclic ring system with between 3 and 14 ring atoms. Said method comprises the production, as starting or intermediate products, of compounds of formula (II) in which R?3 and R4¿ are readily cleavable groups and R?1 and R2¿ have the meanings given above. Said compounds are cyclized under suitable reaction conditions to yield compounds of formula (I).

公开(公告)号：EP1501788B1

公开(公告)日：2010-04-14

申请号：EP03720529.1

申请日：2003-04-25

Applicant: BASF SE

Inventor： ENGEL, Stefan ,  KEIL, Michael ,  OTT, Christian ,  RACK, Michael

IPC: C07C253/30 ,  C07C255/56

CPC classification number: C07C253/30 ,  C07C255/56

Abstract: The invention relates to a method for producing 3-trifluoromethylphenyl-4-cyanobenzyl ketone by reacting a 3-trifluoromethyl benzoic acid-C1-C2-alkyl ester with 4-tolunitrile in an aprotic polar solvent or in an aprotic polar solvent mixture in the presence of at least one equimolar quantity of a base, whereby the base is selected among potassium alcoholates of primary C1-C4 alkanols.

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

Applicant: BASF SE

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

IPC: C07D237/04 ,  C07F7/04

CPC classification number: C07D231/14

Abstract: 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.