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1. 发明授权

US07847097B2 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：US07847097B2
公开(公告)日：2010-12-07
申请号：US11913208
申请日：2006-05-18
申请人： Joachim Gebhardt , Sandra Loehr , Michael Keil , Thomas Schmidt , Jan Hendrik Wevers , Helmut Zech , Rudolf Haeberle
发明人： Joachim Gebhardt , Sandra Loehr , Michael Keil , Thomas Schmidt , Jan Hendrik Wevers , Helmut Zech , Rudolf Haeberle
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-苯基尿嘧啶和式III的1-烷基化剂R1- L1 III，彼此之间，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。

2. 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。

3. 发明授权

US08124818B2 Method for the production of 3-phenyl(thio) uracils and dithiouracils 有权
标题翻译：制备3-苯基（硫代）尿嘧啶和二硫尿嘧啶的方法
公开(公告)号：US08124818B2
公开(公告)日：2012-02-28
申请号：US13040292
申请日：2011-03-04
申请人： Sandra Loehr , Joachim Gebhardt , Guido Mayer , Michael Keil , Thomas Schmidt , Bernd Wolf
发明人： Sandra Loehr , Joachim Gebhardt , Guido Mayer , Michael Keil , Thomas Schmidt , Bernd Wolf
IPC分类号： C07C15/00
CPC分类号： C07D239/54
摘要： The present invention relates to a process for preparing 3-phenyl(thio)uracils and -dithiouracils of the formula I where the variables are each as defined in the description, and also intermediates for their preparation.
摘要翻译：本发明涉及一种制备式I的3-苯基（硫代）尿嘧啶和二硫尿嘧啶的方法，其中各变量各自如说明书中所定义，以及它们制备的中间体。

4. 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.

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