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81. 发明申请

US20110009640A1 BIFUNCTIONAL PHENYL ISO (THIO) CYANATES, PROCESSES AND INTERMEDIATES FOR THEIR PREPARATION 有权
标题翻译：双功能苯乙烯（THIO）氰化物，其制备方法和中间体
公开(公告)号：US20110009640A1
公开(公告)日：2011-01-13
申请号：US12886986
申请日：2010-09-21
申请人： Gerhard Hamprecht , Michael Puhl , Bernd Wolf , Norbert Götz , Michael Keil , Robert Reinhard , Ingo Sagasser , Werner Seitz
发明人： Gerhard Hamprecht , Michael Puhl , Bernd Wolf , Norbert Götz , Michael Keil , Robert Reinhard , Ingo Sagasser , Werner Seitz
IPC分类号： C07D249/14 , C07C263/10 , C07C331/28 , C07C265/12 , C07D249/12 , C07C307/02
CPC分类号： C07D213/76 , C07C303/34 , C07C307/06 , C07C331/28 , C07C2601/14 , C07D207/20 , C07D211/18 , C07D211/70 , C07D295/26 , C07D307/52 , C07D319/06 , C07D333/20
摘要： A process for preparing phenyl iso(thio)cyanates of the formula I in which a compound of the formula II or its HCl adduct is reacted with a phosgenating agent where W is oxygen or sulfur and Ar and A are as defined in claim 1 is described.Moreover, the invention relates to the use of the phenyl iso(thio)cyanates for preparing crop protection agents.
摘要翻译：描述式I的苯基异（硫代）氰酸酯的方法，其中将式II化合物或其HCl加合物与W是氧或硫的光气反应剂和Ar和A如权利要求1中所定义的相同。此外，本发明涉及苯基异（硫代）氰酸酯用于制备作物保护剂的用途。

82. 发明申请

US20100256418A1 PROCESS FOR PREPARING SUBSTITUTED BIPHENYLS 有权
标题翻译：制备替代BIPHENYLS的方法
公开(公告)号：US20100256418A1
公开(公告)日：2010-10-07
申请号：US12726196
申请日：2010-03-17
申请人： Sebastian Peer SMIDT , Jochen Dietz , Michael Keil , Thomas Grote
发明人： Sebastian Peer SMIDT , Jochen Dietz , Michael Keil , Thomas Grote
IPC分类号： C07C205/04
CPC分类号： C07C201/12 , C07C209/68 , C07C211/52 , C07C205/12
摘要： A process for preparing substituted biphenyls of the formula I in which the substituents are defined as follows: X is fluorine or chlorine; R1 is nitro, amino or NHR3; R2 is cyano, nitro, halogen, C1-C6-alkyl, C1-C-6-alkenyl, C1-C6-alkynyl, C1-C6-alkoxy, C1-C6-haloalkyl, C1-C6-alkylcarbonyl or phenyl; R3 is C1-C4-alkyl, C1-C4-alkenyl or C1-C4-alkynyl; n is 1, 2 or 3, where in case that n is 2 or 3, the R.sup.2 radicals may also be different, which comprises reacting the compound of the formula II in which Hal is halogen and X and R1 are as defined above, in the presence of a base and of a palladium catalyst selected from the group of:3 a) palladium-triarylphosphine or -trialkylphosphine complex with palladium in the zero oxidation state, b) salt of palladium in the presence of triarylphospine or trialkylphosphine as a complex ligand or c) metallic palladium, optionally applied to support, in the presence of triarylphosphine or trialkylphosphine, in a solvent, with a diphenylborinic acid (III) in which R2 and n are as defined above, where the triarylphosphines or trialkylphosphines used may be substituted.
摘要翻译：制备式I取代的联苯的方法，其中取代基定义如下：X是氟或氯; R1是硝基，氨基或NHR3; R2是氰基，硝基，卤素，C1-C6-烷基，C1-C6-6烯基，C1-C6-炔基，C1-C6-烷氧基，C1-C6-卤代烷基，C1-C6烷基羰基或苯基; R3是C1-C4-烷基，C1-C4-烯基或C1-C4-炔基; n为1,2或3，其中在n为2或3的情况下，R 2基团也可以不同，其包括使其中Hal为卤素且X和R 1的式II化合物与在碱存在下和选自以下组中的钯催化剂存在下：a）钯 - 三芳基膦或三烷基膦配合物与钯在零氧化状态，b）钯在三芳基膦或三烷基膦存在下的盐作为络合配体或c）金属钯，任选地在三芳基膦或三烷基膦存在下，在溶剂中与二苯基硼酸（III）反应，其中R 2和n如上所定义，其中使用三芳基膦或三烷基膦可以被替代。

83. 发明申请

US20100228054A1 Method for Producing Sulfonamides 失效
标题翻译：生产磺酰胺的方法
公开(公告)号：US20100228054A1
公开(公告)日：2010-09-09
申请号：US12095582
申请日：2006-11-23
申请人： Michael Keil , Joachim Gebhardt , Michael Rack , Guido Mayer , Thomas Schmidt , Jan Hendrik Wevers , Sandra Lohr , Axel Pleschke
发明人： Michael Keil , Joachim Gebhardt , Michael Rack , Guido Mayer , Thomas Schmidt , Jan Hendrik Wevers , Sandra Lohr , Axel Pleschke
IPC分类号： C07C307/00 , C07C311/00 , C07C205/06
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，其中变量具有在本说明书中引用的名称，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，将式III的氨基磺酸与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式Ⅱ和B2当量的碱基IV; B，B1和B2具有说明书中引用的标号。

84. 发明申请

US20100105562A1 Crystalline Form of 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)-pyrimidinyl]-4-fluoro-N-[[methyl(1-methylethyl)amino]sulfonyl]benzamide 有权
标题翻译： 2-氯-5- [3,6-二氢-3-甲基-2,6-二氧代-4-（三氟甲基）-1-（2H） - 嘧啶基] -4-氟-N - [[甲基（1-甲基乙基）氨基]磺酰基]苯甲酰胺
公开(公告)号：US20100105562A1
公开(公告)日：2010-04-29
申请号：US12444653
申请日：2007-10-12
申请人： Thomas Schmidt , Joachim Gebhardt , Sandra Löhr , Michael Keil , Jan Hendrik Wevers , Peter Erk , Heidi Emilia , Gerhard Hamprecht , Werner Seitz , Guido Mayer , Bernd Wolf , Gerhard Cox , Alfred Michel , Cyrill Zagar , Robert Reinhard , Bernd Sievernich
发明人： Thomas Schmidt , Joachim Gebhardt , Sandra Löhr , Michael Keil , Jan Hendrik Wevers , Peter Erk , Heidi Emilia , Gerhard Hamprecht , Werner Seitz , Guido Mayer , Bernd Wolf , Gerhard Cox , Alfred Michel , Cyrill Zagar , Robert Reinhard , Bernd Sievernich
IPC分类号： A01N43/54 , C07D239/54 , A01P13/00
CPC分类号： C07D239/54
摘要： The present invention relates to a crystalline form of 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)pyrimidinyl]-4-fluoro-N-[[methyl(1-methylethyl)-amino]sulfonyl]benzamide. The invention also relates to a process for the preparation of this crystalline form and to plant protection formulations which comprise this crystalline form of the phenyluracil.
摘要翻译：本发明涉及2-氯-5- [3,6-二氢-3-甲基-2,6-二氧代-4-（三氟甲基）-1-（2H）嘧啶基] -4-氟 - N - [[甲基（1-甲基乙基） - 氨基]磺酰基]苯甲酰胺。本发明还涉及制备该结晶形式的方法以及包含该苯基尿嘧啶的该结晶形式的植物保护制剂。

85. 发明申请

US20100056820A1 Method for the production of substituted 2-aryl malonic acid esters 审中-公开
标题翻译：制备取代的2-芳基丙二酸酯的方法
公开(公告)号：US20100056820A1
公开(公告)日：2010-03-04
申请号：US12522211
申请日：2008-01-21
申请人： Volker Maywald , Christian Ott , Bernd Wolf , Manfred Ehresmann , Michael Rack , Michael Keil , Sebastian Peer Smidt
发明人： Volker Maywald , Christian Ott , Bernd Wolf , Manfred Ehresmann , Michael Rack , Michael Keil , Sebastian Peer Smidt
IPC分类号： C07C69/34
CPC分类号： C07C17/12 , C07C67/343 , C07C25/13 , C07C69/65
摘要： The present invention relates to a process for preparing substituted 2-arylmalonic esters of the general formula I in which R is C1-C6-alkyl or C1-C4-alkoxy-C1-C4-alkyl; Ar is phenyl or a heteroaromatic 5- or 6-membered ring; where each carbon atom present in the radicals mentioned above optionally carries a substituent RA; RA is F, Cl, CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, etc., or two adjacent substituents RA together with the carbon atoms to which they are attached form a ring; and where a malonic ester is reacted with a base and an aryl bromide in the presence of a copper salt, which comprises employing from 0.1 to 0.65 molar equivalents of the base per molar equivalent of the malonic ester.
摘要翻译：本发明涉及制备通式Ⅰ的取代的2-芳基丙二酸酯的方法，其中R是C 1 -C 6 - 烷基或C 1 -C 4 - 烷氧基-C 1 -C 4烷基; Ar是苯基或杂芳族5或6元环; 其中存在于上述基团中的每个碳原子任选地带有取代基RA; RA是F，Cl，CN，NO 2，C 1 -C 4 - 烷基，C 1 -C 4卤代烷基，C 1 -C 4 - 烷氧基，C 1 -C 4 - 卤代烷氧基等，或两个相邻的取代基RA与它们连接形成环; 并且其中丙二酸酯在铜盐存在下与碱和芳基溴反应，其包括使用每摩尔当量丙二酸酯0.1至0.65摩尔当量的碱。

86. 发明授权

US07663001B2 Preparation of isoxazolin-3-ylacylbenzene 有权
标题翻译：异恶唑啉-3-基酰基苯的制备
公开(公告)号：US07663001B2
公开(公告)日：2010-02-16
申请号：US11684630
申请日：2007-03-11
申请人： Joachim Rheinheimer , Wolfgang von Deyn , Joachim Gebhardt , Michael Rack , Rene Lochtman , Norbert Götz , Michael Keil , Matthias Witschel , Helmut Hagen , Ulf Miβlitz , Ernst Baumann
发明人： Joachim Rheinheimer , Wolfgang von Deyn , Joachim Gebhardt , Michael Rack , Rene Lochtman , Norbert Götz , Michael Keil , Matthias Witschel , Helmut Hagen , Ulf Miβlitz , Ernst Baumann
IPC分类号： C07C239/08
CPC分类号： C07C249/06 , C07C201/10 , C07C201/12 , C07C205/44 , C07C209/62 , C07C251/48 , C07C253/00 , C07C255/50 , C07C315/04 , C07C319/14 , C07D261/04 , C07D413/10 , C07C323/09 , C07C317/24 , C07C317/32 , C07C205/06 , C07C211/52
摘要： A process is described for preparing isoxazoles of the formula I where the substituents are as defined below: R1 is hydrogen, C1-C6-alkyl, R2 is C1-C6-alkyl, R3, R4, R5 are hydrogen, C1-C6-alkyl, or R4 and R5 together form a bond, R6 is a heterocyclic ring, n is 0, 1 or 2; which comprises preparing an intermediate of the formula VI where R1, R3, R4 and R5 are as defined above, followed by halogenation, thiomethylation, oxidation and acylation to give compounds of the formula I. Also novel intermediates for preparing the compounds of the formula I and novel processes for preparing the intermediates are described.
摘要翻译：描述了制备式I的异恶唑的方法，其中取代基如下所定义：R 1是氢，C 1 -C 6烷基，R 2是C 1 -C 6烷基，R 3，R 4，R 5是氢，C 1 -C 6 - 烷基，或R4和R5一起形成键，R6是杂环，n是0,1或2; 其包括制备式VI的中间体，其中R 1，R 3，R 4和R 5如上定义，然后进行卤化，硫甲基化，氧化和酰化，得到式I化合物。还有用于制备式I化合物的中间体并描述了制备中间体的新方法。

87. 发明授权

US07595426B2 Method for the production of 1,3,5-trifluoro-2,4,6-trichlorobenzene from fluorobenzene derivatives 失效
标题翻译：从氟苯衍生物制备1,3,5-三氟-2,4,6-三氯苯的方法
公开(公告)号：US07595426B2
公开(公告)日：2009-09-29
申请号：US11911971
申请日：2006-04-21
申请人： Michael Rack , Sebastian Peer Smidt , Manuel Budich , Volker Maywald , Michael Keil , Bernd Wolf
发明人： Michael Rack , Sebastian Peer Smidt , Manuel Budich , Volker Maywald , Michael Keil , Bernd Wolf
IPC分类号： C07C22/00 , C07C17/00
CPC分类号： C07C25/13 , C07C17/12 , C07C17/208 , C07C17/23
摘要： Method for the production of 1,3,5-trifluoro-2,4,6-trichlorobenzene from fluorobenzene comprising steps A) and B): A) chlorination of fluorobenzene derivatives of formula (II), in which X=fluorine of H, Z=nitro, bromo or chloro and n=0 or 1-4 and B) fluorination of the distillation residue and separation by distillation of the 1,3,5-trifluoro-2,4,6-trichlorobenzene thus produced.
摘要翻译：由氟代苯制备1,3,5-三氟-2,4,6-三氯苯的方法，包括步骤A）和B）：A）氯化式（II）的氟代苯衍生物，其中X = H的氟， Z =硝基，溴或氯，n = 0或1-4，B）氟化蒸馏残余物并通过蒸馏分离由此制得的1,3,5-三氟-2,4,6-三氯苯。

88. 发明授权

US07488840B2 Method for producing 2-chloromethylphenyl acetic acid derivatives 失效
标题翻译： 2-氯甲基苯基乙酸衍生物的制备方法
公开(公告)号：US07488840B2
公开(公告)日：2009-02-10
申请号：US10505475
申请日：2003-02-06
申请人： Guido Mayer , Oliver Cullmann , Bernd Wolf , Michael Keil , Wassilios Grammenos
发明人： Guido Mayer , Oliver Cullmann , Bernd Wolf , Michael Keil , Wassilios Grammenos
IPC分类号： C07C229/00 , C07C241/00
CPC分类号： C07C249/12 , C07C251/48
摘要： The invention relates to a method for producing 2-chloromethylphenyl acetic acid derivatives of formula (I), in which X represents C1-C4 alkoxy or methylamino, by cleaving the ether bonds in compounds of formula (II), in which R represents C1-C4 alkyl, C1-C4 alkoxy, C1-C2 alkyl halide, C1-C4 alkylcarbonyl, C1-C4 alkylcarbonyloxy, halogen, nitro or cyano, and X has the above-mentioned meaning. The inventive method is characterized in that the transformation takes place in the presence of hydrogen chloride and of an inert solvent, and in that a catalyst selected from the group comprised of: iron, indium or halogenides, oxides or triflates thereof is added to the reaction mixture.
摘要翻译：本发明涉及通过在式（II）化合物中切割醚键而制备式（I）的2-氯甲基苯基乙酸衍生物的方法，其中X代表C1-C4烷氧基或甲基氨基，其中R表示C1- C4烷基，C1-C4烷氧基，C1-C2烷基卤，C1-C4烷基羰基，C1-C4烷基羰基氧基，卤素，硝基或氰基，X具有上述含义。本发明的方法的特征在于转化是在氯化氢和惰性溶剂的存在下进行的，其中将选自铁，铟或卤化物，氧化物或三氟甲磺酸酯的催化剂加入到反应中混合物。

89. 发明申请

US20080200675A1 Method for Production of Substituted Phenylmalonate Esters, Novel Phenylmalonate Esters and Use Thereof 审中-公开
标题翻译：替代苯丙糖酸酯的生产方法，新型苯丙二酸酯及其用途
公开(公告)号：US20080200675A1
公开(公告)日：2008-08-21
申请号：US11993947
申请日：2006-06-23
申请人： Norbert Gotz , Volker Maywald , Michael Keil
发明人： Norbert Gotz , Volker Maywald , Michael Keil
IPC分类号： C07C69/76 , C07D487/00
CPC分类号： C07C67/31 , C07C67/00 , C07C67/343 , C07C69/734 , C07D471/04 , C07C69/65
摘要： A process for preparing substituted phenylmalonic esters of the formula in which R is alkyl and Q is halogen, alkyl, alkoxy, haloalkyl or haloalkoxy and the index m is an integer from 1 to 5, where the groups Q can be identical or different if the index m is greater than 1, comprising steps A), B) and C):A) reaction of compounds of the formula II, in which the variables are as defined for formula I to give compounds of the formula III, B) conversion of the compounds of the formula III into ketals of the formula IV in which R′ is C1-C4-alkyl or benzyl,C) hydrolysis of the compounds of the formula IV to give compounds of the formula I;novel phenylmalonic ester derivatives, and their use as intermediates.
摘要翻译：制备下式的取代苯基丙二酸酯的方法，其中R是烷基，Q是卤素，烷基，烷氧基，卤代烷基或卤代烷氧基，并且指数m是1至5的整数，其中基团Q可以相同或不同，如果指数m大于1，包括步骤A），B）和C）：A）式II化合物的反应，其中变量如式I所定义，得到式III化合物，B）式III的化合物转化成式IV的缩酮，其中R'是C 1 -C 4 - 烷基或苄基，C）式 IV，得到式I化合物; 新型苯基丙二酸酯衍生物及其作为中间体的用途。

90. 发明授权

US06727385B1 Method for producing o-chloromethyl benzoic acid chlorides 失效
标题翻译：邻氯甲基苯甲酸氯化物的生产方法
公开(公告)号：US06727385B1
公开(公告)日：2004-04-27
申请号：US10130825
申请日：2002-08-12
申请人： Roland Götz , Norbert Götz , Michael Keil , Bernd Wolf , Adrian Steinmetz , Armin Stamm , Jochem Henkelmann
发明人： Roland Götz , Norbert Götz , Michael Keil , Bernd Wolf , Adrian Steinmetz , Armin Stamm , Jochem Henkelmann
IPC分类号： C07C5536
CPC分类号： C07C51/60 , C07C63/04 , C07C63/10
摘要： A process for preparing o-chloromethylbenzoyl chlorides of the formula I, in which R1 to R4 can be identical or different and are hydrogen, C1-C4-alkyl, halogen or trifluoromethyl, by reacting benzo-fused lactones of the formula II, in which R1 to R4 are as defined above, with thionyl chloride, which comprises carrying out the reaction in the presence of catalytic amounts of boric acid, boric anhydride, borate, boronic acid or boronic acid esters and catalytic amounts of a quaternary ammonium salt is described.
摘要翻译：制备式I的邻氯甲基苯甲酰氯的方法，其中R 1至R 4可以相同或不同，并且是氢，C 1 -C 4 - 烷基，卤素或三氟甲基，通过使苯并稠合的内酯与其中R 1至R 4如上所定义的式II与亚硫酰氯反应，其包括在催化量的硼酸，硼酸酐，硼酸盐，硼酸或硼酸的存在下进行反应描述了酯和催化量的季铵盐。

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