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1. 发明公开

EP3359512A1 PROCESS FOR THE PREPARATION OF ORGANIC BROMIDES 审中-公开
公开(公告)号：EP3359512A1
公开(公告)日：2018-08-15
申请号：EP16853205.9
申请日：2016-10-06
申请人： Technion Research & Development Foundation Limited
发明人： GANDELMAN, Mark , NISNEVICH, Gennady A. , KULBITSKI, Kseniya , ARTARYAN, Alexander
IPC分类号： C07C17/363 , C07C22/04 , C07C25/02 , C07C23/10
CPC分类号： C07C17/363 , C07B39/00 , C07C19/075 , C07C23/10 , C07C25/02 , C07C41/22 , C07C45/676 , C07C67/32 , C07C201/12 , C07C253/30 , C07C255/65 , C07C409/34 , C07C2601/04 , C07C2601/14 , C07C2602/42 , C07C2603/74 , C07C2603/90 , C07D205/04 , C07D209/48 , C07D211/38 , C07J9/005 , C07C25/13 , C07C22/04 , C07C22/00 , C07C205/12 , C07C255/50 , C07C205/58 , C07C69/76 , C07C69/63 , C07C43/225 , C07C69/74 , C07C69/753 , C07C49/477
摘要： The present invention provides a process for the preparation of organic bromides, by a radical bromodecarboxylation of carboxylic acids with a bromoisocyanurate.

2. 发明公开

EP3168224A1 ORGANOZINC COMPOSITION 审中-公开
标题翻译：有机锌组合物
公开(公告)号：EP3168224A1
公开(公告)日：2017-05-17
申请号：EP15194823.9
申请日：2015-11-16
申请人： Ludwig-Maximilians-Universität München
发明人： Knochel, Paul , Becker, Matthias
IPC分类号： C07F19/00 , C07F3/06 , C07B37/04 , C07C201/12 , C07D239/30
CPC分类号： C07F19/005 , C07B37/04 , C07C201/12 , C07C253/30 , C07D213/61 , C07D239/30 , C07D307/68 , C07D333/40 , C07D473/40 , C07F3/06 , C07C205/58 , C07C205/35 , C07C215/56 , C07C255/50 , C07C255/57 , C07C255/54
摘要： The present invention relates to compositions containing a zinc complex wherein a zinc atom carries two amide ligands, a lithium salt and a defined solvent. The compositions are stable and show high activity as reactants for metalation reactions, and thus provide a valuable tool in organic synthesis. Moreover, the invention relates to processes for the preparation of the compositions and to synthetic procedures using them.
摘要翻译：本发明涉及含锌配合物的组合物，其中锌原子携带两个酰胺配体，锂盐和限定的溶剂。该组合物是稳定的并且显示出作为金属化反应的反应物的高活性，并因此提供了有机合成中的有价值的工具。此外，本发明涉及制备组合物的方法和使用它们的合成方法。

3. 发明公开

EP3015451A1 METHOD FOR MANUFACTURING NITROBENZENE COMPOUND 有权
标题翻译： VERFAHREN ZUR HERSTELLUNG EINER NITROBENZOLVERBINDUNG
公开(公告)号：EP3015451A1
公开(公告)日：2016-05-04
申请号：EP14817123.4
申请日：2014-06-03
申请人： Ihara Chemical Industry Co., Ltd.
发明人： IKUMI, Akiko , NAKAMURA, Takayuki
IPC分类号： C07C201/06 , C07C205/12 , C07C205/58 , C07B61/00
CPC分类号： C07C201/10 , C07C205/58 , C07C205/12
摘要： The purpose of the present invention is to provide an economically favorable, industrialization-suitable method for manufacturing nitrobenzene compounds of general formula (1). A method for manufacturing nitrobenzene compounds of general formula (1):

(in the formula, R 1 represents a halogen atom; R 2 , R 3 , and R 4 represent a hydrogen atom, etc.; and R 5 represents a halogen atom or alkoxy carbonyl group), the method including the following processes: (i) a process for reacting aniline compounds of general formula (2):

(in the formula, R 1 , R 2 , R 3 , R 4 , and R 5 are as previously defined.) in the presence of a metal salt of nitrous acid and an acid, and (ii) a process for reacting the product of process (i) in the presence of a metal salt of nitrous acid and a copper compound; and the total amount of water used in process (ii) being 1.2-2.2 L (liters) with respect to one mole of the compound of general formula (2).
摘要翻译：本发明的目的是提供一种经济上有利的工业化合适的制备通式（1）的硝基苯化合物的方法。制备通式（1）的硝基苯化合物的方法：（式中，R 1表示卤素原子; R 2，R 3和R 4表示氢原子等; R 5表示卤素原子或烷氧基羰基），该方法包括以下方法：（i）使通式（2）的苯胺化合物反应的方法：（式中，R 1，R 2，R 3，R 4和R 5为（ii）在亚硝酸金属盐和铜化合物的存在下使方法（i）的产物反应的方法;和（ii）使方法（i）的产物在亚硝酸金属盐和铜化合物的存在下反应的方法; 并且相对于1摩尔通式（2）的化合物，方法（ii）中使用的水的总量为1.2-2.2L（升）。

4. 发明公开

EP2754651A4 NITROBENZENE COMPOUND MANUFACTURING METHOD 有权
标题翻译：的连接方法硝基苯
公开(公告)号：EP2754651A4
公开(公告)日：2015-03-11
申请号：EP12807434
申请日：2012-07-04
申请人： IHARA CHEMICAL IND CO
发明人： TANI SHINKI , YADOMATSU NAMI , IKUMI AKIKO , HIRANO YUUKI , IDO TAKUYA
IPC分类号： C07C201/06 , C07B61/00 , C07C205/06 , C07C227/08 , C07C229/56
CPC分类号： C07C201/06 , C07C205/06 , C07C205/58
摘要： There is provided a method for producing a nitrobenzene compound that can be implemented by a simple operation under mild conditions without using a special reaction apparatus. [Solution] The present invention provides a method for producing a nitrobenzene compound represented by general formula (2), wherein R 1 and R 5 are the same or different, and each is a halogen atom or another functional group, and R 2 , R 3 , and R 4 are the same or different, and each is a hydrogen atom or another functional group, comprising oxidizing an aniline compound represented by general formula (1), wherein R 1 , R 2 , R 3 , R 4 , and R 5 are the same as described above, with hydrogen peroxide in the presence of a tungsten compound under an acidic condition, followed by oxidation with hydrogen peroxide under a neutral to alkaline condition.

5. 发明公开

EP2474536A4 PROCESS FOR PREPARATION OF PYRIMIDINYLACETONITRILE DERIVATIVES AND INTERMEDIATES FOR SYNTHESIS THEREOF 有权
标题翻译：用于生产PYRIMIDINYLACETONITRILDERIVATEN和中间产品及其合成
公开(公告)号：EP2474536A4
公开(公告)日：2013-02-13
申请号：EP10811488
申请日：2010-08-23
申请人： IHARA CHEMICAL IND CO
发明人： KAWAZOE KENTARO
IPC分类号： C07D239/52 , C07C201/08 , C07C201/12 , C07C205/19 , C07C205/26 , C07C205/34 , C07C205/58
CPC分类号： C07D239/52 , C07C201/08 , C07C201/12 , C07C205/19 , C07C205/34 , C07C205/58

6. 发明公开

EP2532650A2 Modulators of ATP-binding cassette transporters 审中-公开
公开(公告)号：EP2532650A2
公开(公告)日：2012-12-12
申请号：EP12152235.3
申请日：2005-06-24
申请人： Vertex Pharmaceuticals Incorporated
发明人： Hadida Ruah, Sarah S. , Hazlewood, Anna R. , Grootenhuis, Peter D. J. , Van Goor, Fredrick F. , Singh, Ashvani K. , Zhou, Jinglan , McCartney, Jason
IPC分类号： C07D209/08 , C07D209/14 , C07D209/18 , C07D209/42
CPC分类号： C07D471/10 , A61K8/4926 , A61K31/04 , A61K31/136 , A61K31/265 , A61K31/27 , A61K31/277 , A61K31/352 , A61K31/403 , A61K31/404 , A61K31/4045 , A61K31/44 , A61K31/47 , A61K31/4709 , A61K31/472 , A61K31/4747 , A61K31/538 , A61K31/5415 , A61K31/55 , A61K45/06 , C07C205/11 , C07C205/58 , C07C209/00 , C07C211/17 , C07C211/50 , C07C211/52 , C07C215/28 , C07C215/70 , C07C215/76 , C07C215/78 , C07C217/76 , C07C217/80 , C07C217/84 , C07C219/34 , C07C229/52 , C07C255/58 , C07C271/20 , C07C311/08 , C07C311/39 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07C2603/74 , C07D209/04 , C07D209/08 , C07D209/12 , C07D209/14 , C07D209/18 , C07D209/20 , C07D209/42 , C07D209/94 , C07D209/96 , C07D213/20 , C07D213/73 , C07D215/227 , C07D215/233 , C07D215/38 , C07D215/56 , C07D217/04 , C07D217/06 , C07D223/16 , C07D265/36 , C07D279/16 , C07D311/58 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , G01N33/48728 , G01N33/5035 , G01N33/566 , G01N33/6872 , G01N2333/705
摘要： The present invention relates to modulators of ATP-Binding Cassette ("ABC") transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, composition thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

7. 发明公开

EP2530075A2 Modulators of ATP-binding cassette transporters 审中-公开
公开(公告)号：EP2530075A2
公开(公告)日：2012-12-05
申请号：EP12152246.0
申请日：2005-06-24
申请人： Vertex Pharmaceuticals Incorporated
发明人： Hadida Ruah, Sarah S. , Hazlewood, Anna R. , Grootenhuis, Peter D. J. , Van Goor, Fredrick F. , Singh, Ashvani K. , Zhou, Jinglan , McCartney, Jason
IPC分类号： C07D209/08 , C07D209/14 , C07D209/42 , C07D213/20 , C07D213/73 , C07D215/38 , C07D215/56 , C07D217/06 , C07D223/16 , C07D279/16 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/10 , C07C215/76 , A61K31/47 , A61K31/4709 , A61P25/00 , A61P31/00
CPC分类号： C07D471/10 , A61K8/4926 , A61K31/04 , A61K31/136 , A61K31/265 , A61K31/27 , A61K31/277 , A61K31/352 , A61K31/403 , A61K31/404 , A61K31/4045 , A61K31/44 , A61K31/47 , A61K31/4709 , A61K31/472 , A61K31/4747 , A61K31/538 , A61K31/5415 , A61K31/55 , A61K45/06 , C07C205/11 , C07C205/58 , C07C209/00 , C07C211/17 , C07C211/50 , C07C211/52 , C07C215/28 , C07C215/70 , C07C215/76 , C07C215/78 , C07C217/76 , C07C217/80 , C07C217/84 , C07C219/34 , C07C229/52 , C07C255/58 , C07C271/20 , C07C311/08 , C07C311/39 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07C2603/74 , C07D209/04 , C07D209/08 , C07D209/12 , C07D209/14 , C07D209/18 , C07D209/20 , C07D209/42 , C07D209/94 , C07D209/96 , C07D213/20 , C07D213/73 , C07D215/227 , C07D215/233 , C07D215/38 , C07D215/56 , C07D217/04 , C07D217/06 , C07D223/16 , C07D265/36 , C07D279/16 , C07D311/58 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , G01N33/48728 , G01N33/5035 , G01N33/566 , G01N33/6872 , G01N2333/705
摘要： The present invention relates to modulators of ATP-Binding Cassette ("ABC") transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, composition thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

8. 发明公开

EP2502902A2 Modulators of ATP-binding cassette transporters 审中-公开
公开(公告)号：EP2502902A2
公开(公告)日：2012-09-26
申请号：EP12152237.9
申请日：2005-06-24
申请人： Vertex Pharmaceuticals Incorporated
发明人： Hadida Ruah, Sarah S. , Hazlewood, Anna R. , Grootenhuis, Peter D. J. , Van Goor, Fredrick F. , Singh, Ashvani K. , Zhou, Jinglan , McCartney, Jason
IPC分类号： C07C215/76 , C07C213/02
CPC分类号： C07D471/10 , A61K8/4926 , A61K31/04 , A61K31/136 , A61K31/265 , A61K31/27 , A61K31/277 , A61K31/352 , A61K31/403 , A61K31/404 , A61K31/4045 , A61K31/44 , A61K31/47 , A61K31/4709 , A61K31/472 , A61K31/4747 , A61K31/538 , A61K31/5415 , A61K31/55 , A61K45/06 , C07C205/11 , C07C205/58 , C07C209/00 , C07C211/17 , C07C211/50 , C07C211/52 , C07C215/28 , C07C215/70 , C07C215/76 , C07C215/78 , C07C217/76 , C07C217/80 , C07C217/84 , C07C219/34 , C07C229/52 , C07C255/58 , C07C271/20 , C07C311/08 , C07C311/39 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07C2603/74 , C07D209/04 , C07D209/08 , C07D209/12 , C07D209/14 , C07D209/18 , C07D209/20 , C07D209/42 , C07D209/94 , C07D209/96 , C07D213/20 , C07D213/73 , C07D215/227 , C07D215/233 , C07D215/38 , C07D215/56 , C07D217/04 , C07D217/06 , C07D223/16 , C07D265/36 , C07D279/16 , C07D311/58 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , G01N33/48728 , G01N33/5035 , G01N33/566 , G01N33/6872 , G01N2333/705
摘要： The present invention relates to modulators of ATP-Binding Cassette ("ABC") transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, composition thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

9. 发明公开

EP1957443A2 VERFAHREN ZUR HERSTELLUNG VON SULFONAMIDEN 审中-公开
公开(公告)号：EP1957443A2
公开(公告)日：2008-08-20
申请号：EP06830101.9
申请日：2006-11-23
申请人： BASF SE
发明人： SCHMIDT, Thomas , GEBHARDT, Joachim , LÖHR, Sandra , KEIL, Michael , WEVERS, Jan Hendrik , RACK, Michael , MAYER, Guido , PLESCHKE, Axel
IPC分类号： C07C303/38 , C07C311/51 , C07C201/12 , C07C205/58 , C07C303/40
CPC分类号： C07C303/38 , C07C201/12 , C07C303/40 , C07C311/51 , C07C205/58
摘要： The invention relates to methods for producing sulfonamides of formula I, wherein the variables have the designations cited in the description, by reacting m-nitro-benzoic acid chlorides of formula II with aminosulfons of formula III, under the influence of B equivalents of base IV. Said method is characterised in that, during step a) the aminosulfon of formula III is reacted with B1 equivalents of base IV, and during step b), the reaction mixture resulting from step a) is reacted with m-nitro-benzoic acid chlorides of formula II and B2 equivalents of base IV; B, B1 and B2 having the designations cited in the description.
摘要翻译：本发明涉及制备式I磺酰胺的方法，其中这些变量在本说明书中引用的名称是通过式B的间硝基 - 苯甲酰氯与式III的氨基砜在B当量的碱IV的影响下反应。所述方法的特征在于，在步骤a）期间，式III的氨基磺与B1当量的碱IV反应，并且在步骤b）期间，将由步骤a）得到的反应混合物与间硝基苯甲酸氯化物碱基IV的式Ⅱ和B2当量; B，B1和B2具有说明书中引用的标号。

10. 发明公开

EP1817283A1 2-SUBSTITUTED INDOLES, THEIR PRECURSORS AND NOVEL PROCESSES FOR THE PREPARATION THEREOF 审中-公开
标题翻译： 2-取代的吲哚，及其前体，新工艺用于生产
公开(公告)号：EP1817283A1
公开(公告)日：2007-08-15
申请号：EP05803043.8
申请日：2005-11-04
申请人： Lautens, Mark , Fang, Yuanqing
发明人： Lautens, Mark , Fang, Yuanqing
IPC分类号： C07D209/24 , C07C205/12 , C07C211/46 , C07D409/04 , C07D401/14 , C07D209/12 , C07D209/08
CPC分类号： C07C205/11 , C07C201/12 , C07C205/58 , C07C211/52 , C07C211/56 , C07D209/08 , C07D209/10 , C07D209/12 , C07D401/04 , C07D409/04 , C07C205/44 , C07C205/45 , C07C205/61
摘要： Disclosed are processes for the preparation of 2-substituted indole compounds wherein the 2-substituent comprises an R4 group, wherein R4 is selected from the group consisting of monocyclic aromatic, polycyclic aromatic, monocyclic heteroaromatic, polycyclic heteroaromatic, 1° alkyl, and alkenyl, all of which are optionally substituted at one or more substitutable positions with one or more suitable substituents, and wherein R4 is bonded to the 2-position of the indole ring via a C-C bond; the process comprising reacting an orthogem-dihalovinylaniline compound of the formula (I): wherein Halo comprises Br, Cl, or I; each of the one or more R1 is independently selected from the group consisting of H, fluoro, lower alkyl, lower alkenyl, lower alkoxy, aryloxy, lower haloalkyl, lower alkenyl, -C(O)O-lower alkyl, monocyclic or polycyclic aryl or heteroaryl moiety, or R1 is an alkenyl group bonded so to as to form a 4- to 20-membered fused monocycle or polycyclic ring with the indole ring; all of which are optionally substituted with one or more suitable substituents at one or more substitutable positions; R2 comprises H, alkyl, cycloalkyl, aryl, heteroaryl, aryl-loweralkyl-, or heteroaryl-loweralkyl-, all of which are optionally substituted at one or more substitutable positions with one or more suitable substituents; R3 comprises H, alkyl, haloalkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycle, aryl-(C1-6)alkyl-, or heteroaryl-loweralkyl-, all of which are optionally substituted at one or more substitutable positions with one or more suitable substituents; with an organoboron reagent selected from the group consisting of a boronic ester of R4, a boronic acid of R4, a boronic acid anhydride of R4, a trialkylborane of R4 and a 9-BBN derivative of R4; in the presence of a base, a palladium metal pre-catalyst and a ligand under reaction conditions effective to form the 2-substituted indole compound. Also disclosed are processes for the preparation of ortho-gem-dihalovinylaniline compounds. Novel compounds prepared by the processes and novel uses of the compounds are likewise disclosed.

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