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61. 发明申请

US20140336404A1 METHOD FOR PRODUCING PENTAFLUOROSULFANYL BENZOIC ACID 有权
标题翻译：生产双酚A苯甲酸的方法
公开(公告)号：US20140336404A1
公开(公告)日：2014-11-13
申请号：US14362779
申请日：2012-12-04
申请人： UBE Industries, Ltd.
发明人： Norimichi Saito , Junichi Chika
IPC分类号： C07C51/04 , C07C63/70
CPC分类号： C07C51/04 , C07C63/70 , C07C381/00
摘要： Provided is a simple, safe, and industrially practical method for producing a pentafluorosulfanylbenzoic acid.This method includes (A) a providing step of providing a trihalomethyl(pentafluorosulfanylbenzene) represented by general formula (1): where X is a halogen atom, n is an integer of 1≦n≦3, and the hydrogen atoms on the benzene ring are optionally replaced with a group having an oxygen atom, a group having a nitrogen atom, or a halogen atom; (B1) a step of reacting the trihalomethyl(pentafluorosulfanylbenzene) with a carboxylic acid, water, or a disiloxane represented by general formula (b): R3Si—O—SiR3 (b) (where R is an alkyl group) in the presence of an acid other than carboxylic acids to form a pentafluorosulfanylbenzoic halide represented by general formula (2a): where X and n are as defined above, and the hydrogen atoms on the benzene ring are optionally replaced with the group or atom defined above; and (B2) a step of converting the pentafluorosulfanylbenzoic halide into a pentafluorosulfanylbenzoic acid represented by general formula (2): where n is as defined above, and the hydrogen atoms on the benzene ring are optionally replaced with the group or atom defined above.
摘要翻译：提供了一种简单，安全和工业上实用的五氟硫烷基苯甲酸的制备方法。该方法包括（A）提供由通式（1）表示的三卤代甲基（五氟硫烷基苯）的提供步骤：其中X是卤素原子，n是1和n1E的整数; n和nlE; 3，苯环上的氢原子任选被具有氧原子的基团，具有氮原子的基团或卤素原子取代; （B1）使通式（b）表示的三卤代甲基（五氟硫烷基苯）与羧酸，水或二硅氧烷反应的步骤：R 3 Si-O-SiR 3（b）（其中R为烷基）除羧酸以外的酸以形成由通式（2a）表示的五氟硫烷基苯甲酰卤：其中X和n如上所定义，苯环上的氢原子任选被上述定义的基团或原子取代; 和（B2）将五氟硫烷基苯甲酸酯转化为由通式（2）表示的五氟硫烷基苯甲酸的步骤：其中n定义如上，苯环上的氢原子任选被上述定义的基团或原子取代。

63. 发明授权

US08642802B2 Process for the preparation of halogenated benzoic acid derivatives 有权
标题翻译：卤代苯甲酸衍生物的制备方法
公开(公告)号：US08642802B2
公开(公告)日：2014-02-04
申请号：US13606052
申请日：2012-09-07
申请人： Stephan Bachmann , Stefan Hildbrand , James Jappy , Dinesh Maganbhai Patel , Christophe Pfleger , Robert John Ernest Tidswell , Rene Trussardi
发明人： Stephan Bachmann , Stefan Hildbrand , James Jappy , Dinesh Maganbhai Patel , Christophe Pfleger , Robert John Ernest Tidswell , Rene Trussardi
IPC分类号： C07C51/16
CPC分类号： C07C45/518 , C07C45/00 , C07C51/15 , C07C51/285 , C07C51/29 , C07C47/55 , C07C63/70
摘要： The present invention comprises a process for the preparation of 3-chloro-2-fluoro-5-trifluoromethyl benzoic acid of the formula or of a salt thereof 3-Chloro-2-fluoro-5-trifluoromethyl benzoic acid or salts thereof are versatile intermediates for the preparation of active pharmaceutical or agrochemical agents.
摘要翻译：本发明包括制备下式的3-氯-2-氟-5-三氟甲基苯甲酸或其盐的方法3-氯-2-氟-5-三氟甲基苯甲酸或其盐是通用的中间体用于制备活性药物或农药。

64. 发明申请

US20130245065A1 INTERMEDIATE COMPOUNDS AND PROCESSES FOR THE PREPARATION OF QUINOLINE DERIVATIVES SUCH AS LAQUINIMOD SODIUM 有权
公开(公告)号：US20130245065A1
公开(公告)日：2013-09-19
申请号：US13989910
申请日：2011-11-28
申请人： Ehud Marom , Michael Mizhiritskii , Shai Rubnov
发明人： Ehud Marom , Michael Mizhiritskii , Shai Rubnov
IPC分类号： C07D215/22 , C07C233/11 , C07C233/55 , C07C63/70
CPC分类号： C07C235/78 , C07C63/70 , C07C229/56 , C07C233/11 , C07C233/55 , C07D215/00 , C07D215/22
摘要： The present invention relates to processes for the preparation of quinoline-3-carboxamide derivatives, such as sodium 5-chloro-3-(ethylphenylcarbamoyl)-1-methyl-2-oxo-1,2-dihydroquinolin-4-olate (Laquinimod sodium). The present invention further relates to intermediates formed in such processes.

65. 发明申请

US20120330055A1 PROCESS FOR THE PREPARATION OF HALOGENATED BENZOIC ACID DERIVATIVES 有权
公开(公告)号：US20120330055A1
公开(公告)日：2012-12-27
申请号：US13606052
申请日：2012-09-07
申请人： Stephan Bachmann , Stefan Hildbrand , James Jappy , Dinesh Maganbhai Patel , Christophe Pfleger , Robert John Ernest Tidswell , Rene Trussardi
发明人： Stephan Bachmann , Stefan Hildbrand , James Jappy , Dinesh Maganbhai Patel , Christophe Pfleger , Robert John Ernest Tidswell , Rene Trussardi
IPC分类号： C07C51/295
CPC分类号： C07C45/518 , C07C45/00 , C07C51/15 , C07C51/285 , C07C51/29 , C07C47/55 , C07C63/70
摘要： The present invention comprises a process for the preparation of 3-chloro-2-fluoro-5-trifluoromethyl benzoic acid of the formula or of a salt thereof 3-Chloro-2-fluoro-5-trifluoromethyl benzoic acid or salts thereof are versatile intermediates for the preparation of active pharmaceutical or agrochemical agents.

66. 发明申请

US20120130121A1 PROCESS FOR THE PREPARATION OF HALOGENATED BENZOIC ACID DERIVATIVES 有权
标题翻译：制备苯甲酸衍生物的方法
公开(公告)号：US20120130121A1
公开(公告)日：2012-05-24
申请号：US13365353
申请日：2012-02-03
申请人： Stephan Bachmann , Stefan Hildbrand , James Jappy , Dinesh Maganbhai Patel , Christophe Pfleger , Robert John Ernest Tidswell , Rene Trussardi
发明人： Stephan Bachmann , Stefan Hildbrand , James Jappy , Dinesh Maganbhai Patel , Christophe Pfleger , Robert John Ernest Tidswell , Rene Trussardi
IPC分类号： C07C51/29 , C07C51/285 , C07C51/305 , C07C51/16
CPC分类号： C07C45/518 , C07C45/00 , C07C51/15 , C07C51/285 , C07C51/29 , C07C47/55 , C07C63/70
摘要： The present invention comprises a process for the preparation of 3-chloro-2-fluoro-5-trifluoromethyl benzoic acid of the formula or of a salt thereof 3-Chloro-2-fluoro-5-trifluoromethyl benzoic acid or salts thereof are versatile intermediates for the preparation of active pharmaceutical or agrochemical agents.
摘要翻译：本发明包括制备下式的3-氯-2-氟-5-三氟甲基苯甲酸或其盐的方法3-氯-2-氟-5-三氟甲基苯甲酸或其盐是通用的中间体用于制备活性药物或农药。

67. 发明授权

US07750182B2 Process for production of iodine compounds and process for production of high-purity 5-iodo-2-methylbenzoic acid 失效
标题翻译：生产碘化合物的方法和生产高纯度5-碘-2-甲基苯甲酸的方法
公开(公告)号：US07750182B2
公开(公告)日：2010-07-06
申请号：US10545005
申请日：2004-02-10
申请人： Toshio Hidaka , Takafumi Yoshimura , Yoshifumi Sato , Norio Fushimi , Masaharu Doya
发明人： Toshio Hidaka , Takafumi Yoshimura , Yoshifumi Sato , Norio Fushimi , Masaharu Doya
IPC分类号： C07C17/00 , C07C63/04
CPC分类号： C07C253/30 , C07B39/00 , C07C17/12 , C07C17/156 , C07C17/158 , C07C51/363 , C07C51/43 , C07C25/02 , C07C25/13 , C07C25/18 , C07C25/125 , C07C63/70 , C07C255/50
摘要： Provided is a production method for an iodine compound in which iodine is reacted with a substrate in the presence of a porous material having a pore diameter of 500 nm or less or in the presence of the above porous material and an oxidizing agent and a production process for high purity 5-iodo-2-methylbenzoic acid comprising an iodination reaction step carried out by the above-mentioned, a crystal precipitation and separation step in which a product is precipitated by adding water or cooling and then separated and a purification step in which crystal separated is recrystallized using an organic solvent. According to the production method for an iodine compound described above, iodine can be introduced into various substrates at a high selectivity. Since expensive metals and specific reagents do not have to be used, it can readily be carried out in an industrially scale, and the product having a high purity can be obtained. Further, the process comprising the iodination reaction, separation and purification steps described above makes it possible to readily obtain at a high yield, 5-iodo-2-methylbenzoic acid having a high purity which is useful in uses for functional chemical products such as medicines. The process of the present invention comprising iodination reaction, separation and purification steps is characterized by that it is simple in terms of a procedure and that the purification load is smaller, and it is very advantageous in industrially carrying out.
摘要翻译：提供一种碘化合物的制造方法，其中碘在孔径为500nm以下的多孔质材料的存在下，或者在上述多孔质材料和氧化剂的存在下，与基材反应，制造方法包括通过上述进行的碘化反应步骤的高纯度5-碘-2-甲基苯甲酸，其中通过加入水或冷却然后分离产物而沉淀产物的晶体沉淀和分离步骤和纯化步骤，其中使用有机溶剂重结晶晶体分离。根据上述碘化合物的制造方法，能够以高选择性将碘引入各种基材中。由于不需要使用昂贵的金属和特定试剂，因此可以容易地以工业规模进行，可以获得高纯度的产物。此外，包括上述碘化反应，分离和纯化步骤的方法使得可以容易地以高产率获得具有高纯度的5-碘-2-甲基苯甲酸，其可用于诸如药物的功能性化学产品的用途。包括碘化反应，分离和纯化步骤的本发明方法的特征在于它在程序方面简单，净化负荷较小，在工业上非常有利。

68. 发明申请

US20090306423A1 PROCESS FOR THE PREPARATION OF HALOGENATED BENZOIC ACID DERIVATIVES 审中-公开
标题翻译：制备苯甲酸衍生物的方法
公开(公告)号：US20090306423A1
公开(公告)日：2009-12-10
申请号：US12474434
申请日：2009-05-29
申请人： Stephan Bachmann , Stefan Hildbrand , James Jappy , Dinesh Maganbhai Patel , Christophe Pfleger , Robert John Ernest Tidswell , Rene Trussardi
发明人： Stephan Bachmann , Stefan Hildbrand , James Jappy , Dinesh Maganbhai Patel , Christophe Pfleger , Robert John Ernest Tidswell , Rene Trussardi
IPC分类号： C07C51/16 , C07C51/00 , C07C51/29
CPC分类号： C07C45/518 , C07C45/00 , C07C51/15 , C07C51/285 , C07C51/29 , C07C47/55 , C07C63/70
摘要： The present invention comprises a process for the preparation of 3-chloro-2-fluoro-5-trifluoromethyl benzoic acid of the formula or of a salt thereof. 3-Chloro-2-fluoro-5-trifluoromethyl benzoic acid or salts thereof are versatile intermediates for the preparation of active pharmaceutical or agrochemical agents.
摘要翻译：本发明包括制备下式的3-氯-2-氟-5-三氟甲基苯甲酸或其盐的方法。 3-氯-2-氟-5-三氟甲基苯甲酸或其盐是用于制备活性药物或农药的多功能中间体。

69. 发明申请

US20080108813A1 PROCESS FOR THE PREPARATION OF 7-SUBSTITUTED 3-ALKYL-3H-ISOBENZOFURAN-1-ONE DERIVATIVES 审中-公开
标题翻译：制备3-取代的3-烷基-3H-异苯并呋喃-1-酮衍生物的方法
公开(公告)号：US20080108813A1
公开(公告)日：2008-05-08
申请号：US11875122
申请日：2007-10-19
申请人： Anita SCHNYDER , Marco PASSAFARO , Thomas RAPOLD
发明人： Anita SCHNYDER , Marco PASSAFARO , Thomas RAPOLD
IPC分类号： C07D239/60 , C07D307/87
CPC分类号： C07D307/88 , C07C63/70
摘要： The present invention relates a process for the preparation of a compound of formula Ia The process includes the step of reacting a first compound having the formula at elevated reaction temperature in the presence of sulfur in a nucleophilic aromatic substitution reaction with an alkali metal sulfide, disulfide or polysulfide of the formula M2Sq wherein R is halogen, R1SO2 or (R1)2NC(X)O; R1 is C1-C8alkyl, aryl-C1-C8alkyl, C1-C8-haloalkyl or aryl; R2 is hydrogen, C1-C4alkyl or C1-C4haloalkyl, X is O or S; and wherein M is an alkali metal or hydrogen, and q is 1, 2 or a fractional number from 1 to 7,
摘要翻译：本发明涉及一种制备式Ia化合物的方法。该方法包括使具有下式的第一种具有式的第一化合物在硫的存在下在升高的反应温度下在亲核芳族取代反应中与碱金属硫化物，二硫化物或多硫化物，其结构式为：α-in-line-formula description =“In-line Formulas”end =“lead”？> M -formulae description =“In-line Formulas”end =“tail”？>其中R是卤素，R 1 SO 2或（R 1）/ SO 2 2）NC（X）O; R 1是C 1 -C 8烷基，芳基-C 1 -C 8烷基， C 1 -C 6烷基，C 1 -C 8 - 卤代烷基或芳基; R 2是氢，C 1 -C 4烷基或C 1 -C 4烷基或C 1 -C 4 - 卤代烷基，X是O或S; 并且其中M为碱金属或氢，q为1,2或1至7的分数，

70. 发明申请

US20070092441A1 Fluoridation method 失效
标题翻译：氟化法
公开(公告)号：US20070092441A1
公开(公告)日：2007-04-26
申请号：US10559878
申请日：2005-04-06
申请人： Harry Wadsworth , Peter Devenish
发明人： Harry Wadsworth , Peter Devenish
IPC分类号： A61K51/00 , C07C25/13 , C07D487/04 , C07D403/02 , C07D401/02
CPC分类号： C07C277/08 , C07B59/001 , C07B2200/05 , C07B2200/11 , C07C17/361 , C07C51/363 , C07C227/16 , C07D209/88 , C07D213/75 , C07D221/20 , C07D231/12 , C07D239/553 , C07D239/95 , C07D401/12 , C07D487/04 , C07C229/36 , C07C279/06 , C07C25/13 , C07C63/70
摘要： A method for the fluoridation of an iodonium salt with a fluoride ion source which can be carried out in an aqueous reaction solvent.
摘要翻译：用氟离子源氟化碘鎓盐的方法，其可以在水性反应溶剂中进行。

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