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11. 发明申请

WO2013024007A1 PROCESS FOR PREPARING N-SUBSTITUTED 1H-PYRAZOLE-5-CARBONYLCHLORIDE COMPOUNDS 审中-公开
标题翻译：制备N-取代的1H-吡唑-5-碳酰氯化合物的方法
公开(公告)号：WO2013024007A1
公开(公告)日：2013-02-21
申请号：PCT/EP2012/065648
申请日：2012-08-10
申请人： BASF SE , KÖRBER, Karsten , DESHMUKH, Prashant , KAISER, Florian , RACK, Michael , FRASSETTO, Timo , VEITCH, Gemma , KORDES, Markus
发明人： KÖRBER, Karsten , DESHMUKH, Prashant , KAISER, Florian , RACK, Michael , FRASSETTO, Timo , VEITCH, Gemma , KORDES, Markus
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-substi- tuted 1 H-pyrazole-5-carbonylchloride compound of the formula (I) comprising the steps of i) deprotonating a compound of the formula (II) 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：本发明涉及一种制备式（I）的N-取代的1H-吡唑-5-碳酰氯化合物的方法，包括以下步骤：i）将式（II）化合物与碱选自具有碳或氮结合的锂的锂有机碱或具有碳键合的镁的镁 - 有机碱; 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。

12. 发明申请

WO2014203185A1 ALKYLATION WITH AN ALKYL FLUOROALKYL SULFONATE 审中-公开
标题翻译：与烷基氟磺酸亚砜的烷基化
公开(公告)号：WO2014203185A1
公开(公告)日：2014-12-24
申请号：PCT/IB2014/062375
申请日：2014-06-18
申请人： NOVARTIS AG , ACEMOGLU, Murat , VEITCH, Gemma
发明人： ACEMOGLU, Murat , VEITCH, Gemma
IPC分类号： C07D498/18 , C07C303/28 , A61K31/436
CPC分类号： C07D498/18 , C07C303/28 , C07F7/1856 , C07C309/65
摘要： The present invention discloses a process for preparing a chemical compound comprising reacting a nucleophile with an alkyl fluoroalkyi sulfonate in the presence of a base of formula NR1 R2R3, wherein R1 and R2 are independently 2-methylpropyl or isopropyl and R3 is - CH(R4)(R5), wherein R4 and R5 are identical or different alkyls that are optionally connected to form a ring. The invention also relates to a process for preparing an alkyl fluoroalkyi sulfonate. The invention further relates to a use of the base in a chemical reaction comprising an alkyl fluoroalkyi sulfonate. The process and uses are suitable for preparing chemical compounds, reactants or intermediates thereof, and in particular for preparing API or reactants, like for example everolimus or reactants for its preparation.
摘要翻译：本发明公开了一种制备化合物的方法，包括在式NR 1 R 2 R 3的碱存在下使亲核体与烷基氟代烷基磺酸酯反应，其中R 1和R 2独立地是2-甲基丙基或异丙基，R 3是-CH（R 4）（R5），其中R4和R5是相同或不同的任选连接形成环的烷基。本发明还涉及制备烷基氟代烷基磺酸盐的方法。本发明还涉及在包含氟代烷基磺酸烷基酯的化学反应中碱的用途。该方法和用途适于制备化合物，反应物或其中间体，特别是用于制备API或反应物，例如依维莫司或其制备的反应物。

13. 发明申请

WO2013076092A1 PROCESS FOR PREPARING N-SUBSTITUTED 1H-PYRAZOLE-5-CARBOXYLATE COMPOUNDS AND DERIVATIVES THEREOF 审中-公开
标题翻译：制备N-取代的1H-吡唑-5-羧酸酯化合物及其衍生物的方法
公开(公告)号：WO2013076092A1
公开(公告)日：2013-05-30
申请号：PCT/EP2012/073128
申请日：2012-11-20
申请人： BASF SE
发明人： DOCHNAHL, Maximilian , KÖRBER, Karsten , DESHMUKH, Prashant , KAISER, Florian , RACK, Michael , FRASSETTO, Timo , VEITCH, Gemma
IPC分类号： C07D401/04 , C07D471/10
CPC分类号： C07D401/04 , C07D471/10
摘要： 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).
摘要翻译：本发明涉及一种制备式（1A）的N-取代的1H-吡唑-5-羧酸酯化合物的方法，包括以下步骤：i）将式（II）的化合物去质子化，其中变量R1，R2 和r各自如说明书和权利要求中所定义，镁 - 有机碱具有碳结合的镁; 和ii）通过使步骤（i）中获得的产物与选自二氧化碳或二氧化碳当量的试剂反应来进行羰基化，得到式（I-A）化合物; 并且涉及进一步转化得到式（I）的N-取代的1H-吡唑-5-碳酰氯化合物。

14. 发明申请

WO2013164295A1 SUBSTITUTED PYRAZOLE-CONTAINING COMPOUNDS AND THEIR USE AS PESTICIDES 审中-公开
标题翻译：取代的含吡唑化合物及其作为杀虫剂的用途
公开(公告)号：WO2013164295A1
公开(公告)日：2013-11-07
申请号：PCT/EP2013/058845
申请日：2013-04-29
申请人： BASF SE , BASF SCHWEIZ AG
发明人： KÖRBER, Karsten , KAISER, Florian , VEITCH, Gemma , VON DEYN, Wolfgang , BANDUR, Nina Gertrud , DICKHAUT, Joachim , NARINE, Arun , CULBERTSON, Deborah L. , NEESE, Paul , GUNJIMA, Koshi
IPC分类号： C07D403/04 , A01N43/00 , A01N57/00 , C07F9/00
CPC分类号： C07D403/04 , A01N43/56 , A01N47/34 , A01N47/36 , A01N57/24 , A01N57/32 , A61K31/506 , A61K31/675 , A61K45/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07F9/247 , C07F9/65583
摘要： The present invention relates to substituted pyrazole-containingcompounds of formula (I), and the stereoisomers and salts thereof, wherein the substituents are as defined in the description. The present invention further relates to a method for combating or controlling invertebrate pests, to a method for protecting plant propagation material and/or the plants which grow therefrom, to plant propagation material comprising at least one compound according to the present invention, to a method for treating or protecting an animal from infestation or infection by parasites, to a process for the preparation of a composition for treating infested or infected animals and/or for protecting animals against infestation or infection by parasites, and to a compound according to the invention for use as a medicament.
摘要翻译：本发明涉及式（I）的取代的含吡唑化合物及其立体异构体和盐，其中取代基如说明书中所定义。本发明还涉及一种防治无脊椎害虫的方法，一种用于保护植物繁殖材料和/或从其生长的植物的方法，包括至少一种根据本发明的化合物的植物繁殖材料的方法，用于治疗或保护动物免受寄生虫感染或感染，涉及制备用于治疗感染或感染的动物和/或保护动物免受寄生虫感染或感染的组合物的方法，以及根据本发明的化合物用作药物。

15. 发明公开

EP2742021A1 ANILINE TYPE COMPOUNDS 审中-公开
标题翻译：苯胺类化合物
公开(公告)号：EP2742021A1
公开(公告)日：2014-06-18
申请号：EP12745699.4
申请日：2012-08-10
申请人： BASF SE
发明人： KÖRBER, Karsten , DESHMUKH, Prashant , KAISER, Florian , RACK, Michael , FRASSETTO, Timo , VEITCH, Gemma , KORDES, Markus , NAUJOK, Marco
IPC分类号： C07C381/10 , C07D401/04 , A01N37/28 , A01N43/56
CPC分类号： A01N43/56 , A01N37/28 , A01N41/12 , A01N43/50 , A01N43/80 , C07B2200/13 , C07C381/10 , C07D401/04 , C07D401/14 , C07D409/14 , C07D413/14
摘要： The present invention relates to compounds of the formula (I) wherein R
1 and R
2 independently of one another are hydrogen, C
1 -C
10 -alkyl, C
1 -C
10 -haloalkyl, C
3 -C
10 -cycloalkyl, C
3 -C
10 -halocycloalkyl, C
2 -C
10 -alkenyl, C
2 -C
10 -haloalkenyl or together represent an aliphatic chain, or the like; R
3 is halogen, cyano, C
1 -C
8 -alkyl, C
1 -C
8 - haloalkyl, C
3 -C
8 -cycloalkyl, C
3 -C
8 -halocycloalkyl, C
2 -C
8 -alkenyl, C
2 -C
8 -haloalkenyl, C
1 -C
8 -alkoxy, phenyl, or the like; R
4 is hydrogen, C
1 -C
10 -alkyl, C
1 -C
10 -haloalkyl, C
3 -C
8 - cycloalkyl, C
3 -C
8 -halocycloalkyl, C
2 -C
10 -alkenyl, C
2 -C
10 -haloalkenyl, phenyl, or the like; t is 0 or 1; p is 0, 1, 2, 3 or 4. The present invention also relates to a process for preparing a compound of the formula (I) which comprises reacting a compound of the formula (II) with a compound of the formulae (III) or (IV): where t, p, R
1 R
3 , R
3 and R
4 are as defined in any of claims 1 to 6 and where A- is an equivalent of an anion having a pΚ
B of at least 10 (determined under standard conditions in water).

16. 发明公开

EP2742023A1 N-THIO-ANTHRANILAMIDE COMPOUNDS AND THEIR USE AS PESTICIDES 审中-公开
标题翻译： N-硫代邻氨基苯甲酰胺化合物及其作为农药
公开(公告)号：EP2742023A1
公开(公告)日：2014-06-18
申请号：EP12748013.5
申请日：2012-08-10
申请人： BASF SE
发明人： KORDES, Markus , DESHMUKH, Prashant , VON DEYN, Wolfgang , KÖRBER, Karsten , DICKHAUT, Joachim , BASTIAANS, Henricus Maria Martinus , KAISER, Florian , NARINE, Arun , BANDUR, Nina Gertrud , VEITCH, Gemma , CULBERTSON, Deborah L. , NEESE, Paul , GUNJIMA, Koshi
IPC分类号： C07D213/60 , C07D213/61 , C07D239/28 , C07D401/04 , A01N43/40
CPC分类号： A01N41/00 , A01N37/46 , A01N43/20 , A01N43/40 , A01N43/54 , A61K31/166 , A61K31/4418 , A61K31/444 , A61K31/506 , C07C381/10 , C07D213/60 , C07D213/61 , C07D239/28 , C07D401/04
摘要： The present invention relates to N-thio-anthranilamide compounds and the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising the same. The invention also relates to the use of the N-thio-anthranilamide compounds or of the compositions comprising such compounds for combating invertebrate pests. Furthermore, the invention relates to methods of applying such compounds.

17. 发明公开

EP2694502A1 SUBSTITUTED PYRIMIDINIUM COMPOUNDS FOR COMBATING ANIMAL PESTS 审中-公开
标题翻译：用于防治动物取代嘧啶化合物
公开(公告)号：EP2694502A1
公开(公告)日：2014-02-12
申请号：EP12711898.2
申请日：2012-04-04
申请人： BASF SE
发明人： DICKHAUT, Joachim , KAISER, Florian , NARINE, Arun , VON DEYN, Wolfgang , KOERBER, Karsten , DESHMUKH, Prashant , VEITCH, Gemma , BANDUR, Nina Gertrud , LANGEWALD, Juergen , CULBERTSON, Deborah L.
IPC分类号： C07D471/04 , A01N43/54 , A61K31/519 , A61P33/10 , A61P33/14
CPC分类号： A01N43/90 , A61K31/519 , C07D471/04 , C07D487/04
摘要： Substituted imine compounds of formula (I), wherein D is C(R
2 )=N∼Z-R
1 or C(=Y
1 )NR
A Y
2 R
B
and the other symbols have the meanings given in the description, their N-oxides and salts are useful for combating animal pests.

18. 发明授权

EP2782910B1 PROCESS FOR PREPARING N-SUBSTITUTED 1H-PYRAZOLE-5-CARBOXYLATE COMPOUNDS AND DERIVATIVES THEREOF 有权
标题翻译： PROCESS FOR制备N-取代的 - 吡唑1H -5-羧酸和它们的衍生物
公开(公告)号：EP2782910B1
公开(公告)日：2016-02-03
申请号：EP12794238.1
申请日：2012-11-20
申请人： BASF SE
发明人： DOCHNAHL, Maximilian , KÖRBER, Karsten , DESHMUKH, Prashant , KAISER, Florian , RACK, Michael , FRASSETTO, Timo , VEITCH, Gemma
IPC分类号： C07D401/04 , C07D471/10
CPC分类号： C07D401/04 , C07D471/10

19. 发明公开

EP2782910A1 PROCESS FOR PREPARING N-SUBSTITUTED 1H-PYRAZOLE-5-CARBOXYLATE COMPOUNDS AND DERIVATIVES THEREOF 有权
标题翻译： PROCESS FOR制备N-取代的 - 吡唑1H -5-羧酸和它们的衍生物
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
申请人： BASF SE
发明人： DOCHNAHL, Maximilian , KÖRBER, Karsten , DESHMUKH, Prashant , KAISER, Florian , RACK, Michael , FRASSETTO, Timo , VEITCH, Gemma
IPC分类号： C07D401/04 , C07D471/10
CPC分类号： C07D401/04 , C07D471/10
摘要： 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).

20. 发明公开

EP2744782A1 CARBAMOYLMETHOXY- AND CARBAMOYLMETHYLTHIO- AND CARBAMOYLMETHYLAMINO BENZAMIDES FOR COMBATING INVERTEBRATE PESTS 审中-公开
标题翻译：氨基甲酰甲氧基 - 和氨基甲酰基甲硫基 - 和氨基甲酰基甲基氨基甲酰胺用于打破无脊椎动物的害虫
公开(公告)号：EP2744782A1
公开(公告)日：2014-06-25
申请号：EP12766286.4
申请日：2012-08-17
申请人： BASF SE
发明人： DESHMUKH, Prashant , KORDES, Markus , VON DEYN, Wolfgang , KÖRBER, Karsten , KAISER, Florian , DICKHAUT, Joachim , NARINE, Arun , BANDUR, Nina Gertrud , VEITCH, Gemma , CULBERTSON, Deborah L. , NEESE, Paul , GUNJIMA, Koshi
IPC分类号： C07D213/61 , A01N43/40
CPC分类号： C07D213/61 , A01N37/28 , A01N43/40 , C07C259/10
摘要： The present invention relates to substituted carbamoylmethoxy and carbamoylmethylthio benzamide compounds (I) and the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising the same. The invention also relates to the use of the carbamoylmethoxy- and carbamoylmethylthio-benzamide compounds or of the compositions comprising such compounds for combating invertebrate pests. Furthermore, the invention relates to methods of applying such compounds.
摘要翻译：本发明涉及取代的氨基甲酰基甲氧基和氨基甲酰基甲硫基苯甲酰胺化合物（I）及其立体异构体，盐，互变异构体和N-氧化物以及包含其的组合物。本发明还涉及氨基甲酰基甲氧基 - 和氨基甲酰基甲硫基 - 苯甲酰胺化合物或包含这些化合物的组合物用于防治无脊椎害虫的用途。此外，本发明涉及施用这种化合物的方法。

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