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1. 发明授权

US08357695B2 Hydrates 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：US08357695B2
公开(公告)日：2013-01-22
申请号：US12444651
申请日：2007-10-12
申请人： Thomas Schmidt , Joachim Gebhardt , Sandra Löhr , Michael Keil , Jan Hendrik Wevers , Peter Erk , Heidi Emilia Saxell , Gerhard Hamprecht , Guido Mayer , Bernd Wolf , Gerhard Cox , Alfred Michel , Werner Seitz , Cyrill Zagar , Robert Reinhard , Bernd Sievernich
发明人： Thomas Schmidt , Joachim Gebhardt , Sandra Löhr , Michael Keil , Jan Hendrik Wevers , Peter Erk , Heidi Emilia Saxell , Gerhard Hamprecht , Guido Mayer , Bernd Wolf , Gerhard Cox , Alfred Michel , Werner Seitz , Cyrill Zagar , Robert Reinhard , Bernd Sievernich
IPC分类号： A01N43/54 , A61K31/505
CPC分类号： C07D239/54 , A01N43/54
摘要： The present invention relates to hydrates 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 these hydrates and to plant protection formulations which comprise hydrates of the phenyluracil I.
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。本发明还涉及制备这些水合物的方法以及包含苯基尿嘧啶I的水合物的植物保护制剂。

2. 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。

3. 发明授权

US08362026B2 Crystalline form of 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)-pyrimidinyl]-4-fluoro-N-[[methyl(1-methyl-ethyl)amino]sulfonyl]benzamide 有权
标题翻译：结晶形式的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：US08362026B2
公开(公告)日：2013-01-29
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 Saxell , 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 Saxell , Gerhard Hamprecht , Werner Seitz , Guido Mayer , Bernd Wolf , Gerhard Cox , Alfred Michel , Cyrill Zagar , Robert Reinhard , Bernd Sievernich
IPC分类号： A01N43/54 , A61K31/505
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。

4. 发明申请

US20100035905A1 Hydrates 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：US20100035905A1
公开(公告)日：2010-02-11
申请号：US12444651
申请日：2007-10-12
申请人： Thomas Schmidt , Joachim Gebhardt , Sandra Löhr , Michael Keil , Jan Hendrik Wevers , Peter Erk , Heidi Emilia Saxell , Gerhard Hamprecht , Guido Mayer , Bernd Wolf , Gerhard Cox , Alfred Michel , Werner Seitz , Cyrill Zagar , Robert Reinhard , Bernd Sievernich
发明人： Thomas Schmidt , Joachim Gebhardt , Sandra Löhr , Michael Keil , Jan Hendrik Wevers , Peter Erk , Heidi Emilia Saxell , Gerhard Hamprecht , Guido Mayer , Bernd Wolf , Gerhard Cox , Alfred Michel , Werner Seitz , Cyrill Zagar , Robert Reinhard , Bernd Sievernich
IPC分类号： A01N43/54 , C07D239/02
CPC分类号： C07D239/54 , A01N43/54
摘要： The present invention relates to hydrates 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 these hydrates and to plant protection formulations which comprise hydrates of the phenyluracil I.
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。本发明还涉及制备这些水合物的方法以及包含苯基尿嘧啶I的水合物的植物保护制剂。

5. 发明申请

US20120310010A1 Method for producing sulfonamides 审中-公开
标题翻译：制备磺酰胺的方法
公开(公告)号：US20120310010A1
公开(公告)日：2012-12-06
申请号：US13584213
申请日：2012-08-13
申请人： Thomas Schmidt , Joachim Gebhardt , Sandra Löhr , Michael Keil , Jan Hendrik Wevers , Michael Rack , Guido Mayer , Axel Pleschke
发明人： Thomas Schmidt , Joachim Gebhardt , Sandra Löhr , Michael Keil , Jan Hendrik Wevers , Michael Rack , Guido Mayer , Axel Pleschke
IPC分类号： C07C303/40 , C07C51/58 , C07C51/60
CPC分类号： C07C303/38 , C07C201/12 , C07C303/40 , C07C311/51 , C07C205/58
摘要： A process for preparing sulfonamides I where the variables are each as defined in the description, by reacting m-nitrobenzoyl chlorides II with amino sulfones III, under the influence of B equivalents of base IV, wherein, in step a), the amino sulfone III is reacted with B1 equivalents of base IV, and, in step b), the reaction mixture resulting from step a) is reacted with m-nitrobenzoyl chlorides II and B2 equivalents of base IV; where B, B1 and B2 are each as defined in the description.
摘要翻译：制备磺酰胺I的方法，其中变量各自如描述中所定义，通过间 - 硝基苯甲酰氯II与氨基砜III在B当量的碱IV的影响下反应，其中在步骤a）中，氨基砜III 与B1当量的碱IV反应，并且在步骤b）中，将由步骤a）得到的反应混合物与间硝基苯甲酰氯II和B 2当量的碱IV反应; 其中B，B1和B2各自如说明书中所定义。

6. 发明授权

US08263806B2 Method for producing sulfonamides 失效
标题翻译：制备磺酰胺的方法
公开(公告)号：US08263806B2
公开(公告)日：2012-09-11
申请号：US12095582
申请日：2006-11-23
申请人： Thomas Schmidt , Joachim Gebhardt , Sandra Löhr , Michael Keil , Jan Hendrik Wevers , Michael Rack , Guido Mayer , Axel Pleschke
发明人： Thomas Schmidt , Joachim Gebhardt , Sandra Löhr , Michael Keil , Jan Hendrik Wevers , Michael Rack , Guido Mayer , Axel Pleschke
IPC分类号： C07C381/00
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 characterized 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。

7. 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。

8. 发明授权

US09920002B2 Methods for producing sulfonic acid diamides 有权
公开(公告)号：US09920002B2
公开(公告)日：2018-03-20
申请号：US12681843
申请日：2008-10-10
申请人： Axel Pleschke , Thomas Schmidt , Joachim Gebhardt , Sandra Loehr , Michael Keil , Jan Hendrik Wevers
发明人： Axel Pleschke , Thomas Schmidt , Joachim Gebhardt , Sandra Loehr , Michael Keil , Jan Hendrik Wevers
IPC分类号： C07C303/34 , C07C307/06 , C07D239/54 , A01N43/54 , C07C381/00
CPC分类号： C07C303/34 , A01N43/54 , C07C307/06 , C07C381/00 , C07D239/54
摘要： The present invention relates to a process for preparing sulfuric diamides of the general formula I R1R2N—S(O)2—NH2 (I) in which R1 and R2 are each independently a primary alkyl radical having from 1 to 8 carbon atoms, a secondary alkyl radical having from 3 to 8 carbon atoms or a cycloalkyl radical having from 5 to 8 carbon atoms, or, together with the nitrogen atom, form a 5- to 8-membered, saturated nitrogen heterocycle which, as well as the nitrogen atom, may have a further heteroatom selected from O and S as a ring member, where the nitrogen heterocycle is unsubstituted or may have 1, 2, 3 or 4 alkyl groups having in each case from 1 to 4 carbon atoms as substituents. The process comprises the following steps: i) the reaction of a secondary amine of the formula II R1R2NH (II) in which R1 and R2 are each as defined above with sulfuryl chloride in an inert solvent, especially an aromatic solvent, in the presence of a tertiary amine to give a sulfamoyl chloride of the formula III R1R2N—S(O)2—Cl (III) in which R1 and R2 are each as defined above, and ii) reaction of the sulfamoyl chloride of the formula III obtained in step i) with ammonia, the sulfamoyl chloride of the formula III being used in step ii) in the form of the solution obtained in step i) in the inert solvent, especially the aromatic solvent.

9. 发明申请

US20080293941A1 Method For Production Of 1-Alkyl-3-Phenyluracils 有权
标题翻译： 1-烷基-3-苯基尿嘧啶的制备方法
公开(公告)号：US20080293941A1
公开(公告)日：2008-11-27
申请号：US11913208
申请日：2006-05-18
申请人： Joachim Gebhardt , Sandra Lohr , Michael Keil , Thomas Schmidt , Jan Hendrik Wevers , Helmut Zech , Rudolf Haberler
发明人： Joachim Gebhardt , Sandra Lohr , Michael Keil , Thomas Schmidt , Jan Hendrik Wevers , Helmut Zech , Rudolf Haberler
IPC分类号： C07D239/54
CPC分类号： C07D239/54
摘要： The present invention relates to a process for preparing 1-alkyl-3-phenyluracils of the formula I where the variables R1 to R7 are as defined in the description by reacting 3-phenyluracils of the formula II and alkylating agents of the formula III R1-L1 III, with one another, wherein during the entire reaction the pH is kept in a range from 1 to 6 by adding base a little at a time.
摘要翻译：本发明涉及一种制备式I的1-烷基-3-苯基尿嘧啶的方法，其中变量R1至R7如说明书中所定义，通过使式II的3-苯基尿嘧啶与式III的烷基化剂反应， in-line-formula description =“In-line Formulas”end =“lead”？> R1-L1 III，<？in-line-formula description =“In-line Formulas”end =“tail”？> ，其中在整个反应期间，通过一次添加碱几乎将pH保持在1至6的范围内。

10. 发明申请

US20100222586A1 Methods for Producing Sulfonic Acid Diamides 有权
标题翻译：生产磺酸二酰胺的方法
公开(公告)号：US20100222586A1
公开(公告)日：2010-09-02
申请号：US12681843
申请日：2008-10-10
申请人： Axel Pleschke , Thomas Schmidt , Joachim Gebhardt , Sandra Loehr , Michael Keil , Jan Hendrik Wevers
发明人： Axel Pleschke , Thomas Schmidt , Joachim Gebhardt , Sandra Loehr , Michael Keil , Jan Hendrik Wevers
IPC分类号： C07D239/10 , C07C309/63
CPC分类号： C07C303/34 , A01N43/54 , C07C307/06 , C07C381/00 , C07D239/54
摘要： The present invention relates to a process for preparing sulfuric diamides of the general formula I R1R2N—S(O)2—NH2 (I) in which R1 and R2 are each independently a primary alkyl radical having from 1 to 8 carbon atoms, a secondary alkyl radical having from 3 to 8 carbon atoms or a cycloalkyl radical having from 5 to 8 carbon atoms, or, together with the nitrogen atom, form a 5- to 8-membered, saturated nitrogen heterocycle which, as well as the nitrogen atom, may have a further heteroatom selected from O and S as a ring member, where the nitrogen heterocycle is unsubstituted or may have 1, 2, 3 or 4 alkyl groups having in each case from 1 to 4 carbon atoms as substituents. The process comprises the following steps: i) the reaction of a secondary amine of the formula II R1R2NH (II) in which R1 and R2 are each as defined above with sulfuryl chloride in an inert solvent, especially an aromatic solvent, in the presence of a tertiary amine to give a sulfamoyl chloride of the formula III R1R2N—S(O)2—Cl (III) in which R1 and R2 are each as defined above, and ii) reaction of the sulfamoyl chloride of the formula III obtained in step i) with ammonia, the sulfamoyl chloride of the formula III being used in step ii) in the form of the solution obtained in step i) in the inert solvent, especially the aromatic solvent.
摘要翻译：本发明涉及制备通式为R 1 R 2 N-S（O）2 -NH 2（I）的硫酸二酰胺的方法，其中R 1和R 2各自独立地为具有1至8个碳原子的伯烷基，二级具有3至8个碳原子的烷基或具有5至8个碳原子的环烷基，或与氮原子一起形成5-8元饱和氮杂环，其氮原子，可以具有选自O和S的另外的杂原子作为环成员，其中氮杂环是未取代的或可以具有1,2,3或4个烷基，每个情况下具有1至4个碳原子作为取代基。该方法包括以下步骤：i）在惰性溶剂，特别是芳族溶剂中，在惰性溶剂，特别是芳族溶剂的存在下，使式II的R 1 R 2 NH（II）的仲胺与R 1和R 2各自如上所述与磺酰氯反应，得到式III的R 1 R 2 N-S（O）2 -C（III）的氨磺酰氯，其中R 1和R 2各自如上所定义，和ii）在步骤（a）中获得的式III的氨磺酰氯的反应， i）与氨，式III的氨磺酰氯以步骤ⅱ）中的步骤i）中获得的溶液的形式在惰性溶剂中，特别是芳族溶剂中使用。

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