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1. 发明申请

US20120065239A1 PROCESS FOR THE PRODUCTION OF AMIDES 有权
标题翻译：生产助剂的方法
公开(公告)号：US20120065239A1
公开(公告)日：2012-03-15
申请号：US13198739
申请日：2011-08-05
申请人： Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi , Fanny Giordano , Martin Zeller , Gottfried Seifert , Shailesh Shah , Neil George , Ian Kevin Jones , Paul Edward Bonnett
发明人： Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi , Fanny Giordano , Martin Zeller , Gottfried Seifert , Shailesh Shah , Neil George , Ian Kevin Jones , Paul Edward Bonnett
IPC分类号： A01N43/56 , A01P3/00 , C07D231/14
CPC分类号： C07C211/61 , A01N43/56 , C07C205/06 , C07C209/325 , C07C209/70 , C07C2603/66 , C07D231/14
摘要： The present invention relates to a process for the preparation of compounds of formula I wherein R1 and R2 are each independently of the other hydrogen or C1-C5alkyl and R3 is CF3 or CF2H, by a) reaction of a compound of formula II wherein R1 and R2 are as defined for formula I, with at least one reducing agent to form a compound of formula wherein R1 and R2 are as defined for formula I, and b) reaction of that compound with at least one reducing agent to form a compound of formula IV wherein R1 and R2 are as defined for formula I, and (c) reaction of that compound with a compound of formula V wherein Q is chlorine, fluorine, bromine, iodine, hydroxy or C1-C6alkoxy and R3 is as defined for formula I, to form the compound of formula I; and to novel intermediates for use in that process.
摘要翻译：本发明涉及一种制备式Ⅰ化合物的方法，其中R1和R2分别独立地为氢或C1-C5烷基，R3为CF3或CF2H，通过a）式II化合物的反应其中R 1和 R 2如式I所定义，与至少一种还原剂形成下式化合物，其中R 1和R 2如式I所定义，和b）该化合物与至少一种还原剂的反应形成式 IV其中R1和R2如式I所定义，和（c）该化合物与式V化合物的反应，其中Q是氯，氟，溴，碘，羟基或C 1 -C 6烷氧基，R 3如式I所定义，形成式I化合物; 以及用于该过程的新型中间体。

2. 发明授权

US07994341B2 Process for the production of amides 有权
标题翻译：酰胺生产工艺
公开(公告)号：US07994341B2
公开(公告)日：2011-08-09
申请号：US12066683
申请日：2006-09-14
申请人： Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi , Fanny Giordano , Martin Zeller , Gottfried Seifert , Shailesh Shah , Neil George , Ian Kevin Jones , Paul Edward Bonnett
发明人： Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi , Fanny Giordano , Martin Zeller , Gottfried Seifert , Shailesh Shah , Neil George , Ian Kevin Jones , Paul Edward Bonnett
IPC分类号： C07D231/14
CPC分类号： C07C211/61 , A01N43/56 , C07C205/06 , C07C209/325 , C07C209/70 , C07C2603/66 , C07D231/14
摘要： The present invention relates to a process for the preparation of compounds of formula (I) wherein R1 and R2 are each independently of the other hydrogen or C1-C5alkyl and R3 is CF3 or CF2H, by a) reaction of a compound of formula (II) wherein R1 and R2 are as defined for formula (I), with at least one reducing agent to form a compound of formula (III) wherein R1 and R2 are as defined for formula (I), and b) reaction of that compound with at least one reducing agent to form a compound of formula (IV) wherein R1 and R2 are as defined for formula (I), and (c) reaction of that compound with a compound of formula (V) wherein Q is chlorine, fluorine, bromine, iodine, hydroxy or C1-C6alkoxy and R3 is as defined for formula (I), to form the compound of formula (I); and to novel intermediates for use in that process.
摘要翻译：本发明涉及制备式（I）化合物的方法，其中R 1和R 2各自独立地为氢或C 1 -C 5烷基，R 3为CF 3或CF 2 H，通过a）式（Ⅱ）化合物）其中R1和R2如式（I）所定义，与至少一种还原剂形成式（III）化合物，其中R 1和R 2如式（I）所定义，和b）该化合物与至少一种还原剂形成式（Ⅳ）化合物，其中R1和R2如式（Ⅰ）所定义，和（c）该化合物与式（Ⅴ）化合物的反应其中Q是氯，氟，溴，碘，羟基或C 1 -C 6烷氧基，R 3如式（I）所定义，形成式（I）化合物; 以及用于该过程的新型中间体。

3. 发明申请

US20090163569A1 PROCESS FOR THE PRODUCTION OF AMIDES 有权
标题翻译：生产助剂的方法
公开(公告)号：US20090163569A1
公开(公告)日：2009-06-25
申请号：US12066683
申请日：2006-09-14
申请人： Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi , Fanny Giordano , Martin Zeller , Gottfried Seifert , Shailesh Shah , Neil George , Ian Kevin Jones , Paul Edward Bonnett
发明人： Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi , Fanny Giordano , Martin Zeller , Gottfried Seifert , Shailesh Shah , Neil George , Ian Kevin Jones , Paul Edward Bonnett
IPC分类号： A01N43/56 , C07D231/14 , C07C211/45 , C07C205/11 , C07D403/12 , A01P7/00
CPC分类号： C07C211/61 , A01N43/56 , C07C205/06 , C07C209/325 , C07C209/70 , C07C2603/66 , C07D231/14
摘要： The present invention relates to a process for the preparation of compounds of formula (I) wherein R1 and R2 are each independently of the other hydrogen or C1-C5alkyl and R3 is CF3 or CF2H, by a) reaction of a compound of formula (II) wherein R1 and R2 are as defined for formula (I), with at least one reducing agent to form a compound of formula (III) wherein R1 and R2 are as defined for formula (I), and b) reaction of that compound with at least one reducing agent to form a compound of formula (IV) wherein R1 and R2 are as defined for formula (I), and (c) reaction of that compound with a compound of formula (V) wherein Q is chlorine, fluorine, bromine, iodine, hydroxy or C1-C6alkoxy and R3 is as defined for formula (I), to form the compound of formula (I); and to novel intermediates for use in that process.
摘要翻译：本发明涉及制备式（I）化合物的方法，其中R 1和R 2各自独立地为氢或C 1 -C 5烷基，R 3为CF 3或CF 2 H，通过a）式（Ⅱ）化合物）其中R1和R2如式（I）所定义，与至少一种还原剂形成式（III）化合物，其中R 1和R 2如式（I）所定义，和b）该化合物与至少一种还原剂形成式（Ⅳ）化合物，其中R1和R2如式（Ⅰ）所定义，和（c）该化合物与式（Ⅴ）化合物的反应其中Q是氯，氟，溴，碘，羟基或C 1 -C 6烷氧基，R 3如式（I）所定义，形成式（I）化合物; 以及用于该过程的新型中间体。

4. 发明授权

US08436037B2 Process for the production of amides 有权
标题翻译：酰胺生产工艺
公开(公告)号：US08436037B2
公开(公告)日：2013-05-07
申请号：US13198739
申请日：2011-08-05
申请人： Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi , Fanny Giordano , Martin Zeller , Gottfried Seifert , Shailesh Shah , Neil George , Ian Jones , Paul Bonnett
发明人： Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi , Fanny Giordano , Martin Zeller , Gottfried Seifert , Shailesh Shah , Neil George , Ian Jones , Paul Bonnett
IPC分类号： A01N43/56 , C07D231/14
CPC分类号： C07C211/61 , A01N43/56 , C07C205/06 , C07C209/325 , C07C209/70 , C07C2603/66 , C07D231/14
摘要： The present invention relates to a process for the preparation of compounds of formula I wherein R1 and R2 are each independently of the other hydrogen or C1-C5alkyl and R3 is CF3 or CF2H, by a) reaction of a compound of formula II wherein R1 and R2 are as defined for formula I, with at least one reducing agent to form a compound of formula III wherein R1 and R2 are as defined for formula I, and b) reaction of that compound with at least one reducing agent to form a compound of formula IV wherein R1 and R2 are as defined for formula I, and (c) reaction of that compound with a compound of formula V wherein Q is chlorine, fluorine, bromine, iodine, hydroxy or C1-C6alkoxy and R3 is as defined for formula I, to form the compound of formula I; and to novel intermediates for use in that process.
摘要翻译：本发明涉及一种制备式Ⅰ化合物的方法，其中R1和R2分别独立地为氢或C1-C5烷基，R3为CF3或CF2H，通过a）式II化合物与式 R 2如式I所定义，与至少一种还原剂形成式III化合物，其中R 1和R 2如式I所定义，和b）该化合物与至少一种还原剂的反应形成式式IV其中R1和R2如式I所定义，和（c）该化合物与式V化合物的反应，其中Q是氯，氟，溴，碘，羟基或C 1 -C 6烷氧基，R 3如式 I，形成式I化合物; 以及用于该过程的新型中间体。

5. 发明授权

US07781615B2 Process for the preparation of amines 有权
标题翻译：制备胺的方法
公开(公告)号：US07781615B2
公开(公告)日：2010-08-24
申请号：US12096796
申请日：2006-12-11
申请人： Hans Tobler , Harald Walter , Camilla Corsi , Josef Ehrenfreund , Fanny Giordano , Martin Zeller
发明人： Hans Tobler , Harald Walter , Camilla Corsi , Josef Ehrenfreund , Fanny Giordano , Martin Zeller
IPC分类号： C07C211/45 , C07C211/48 , C07C209/10 , C07C209/68 , C07C17/266 , C07C25/22
CPC分类号： C07C209/62 , C07B2200/09 , C07C17/23 , C07C17/30 , C07C17/354 , C07C25/22 , C07C25/24 , C07C209/10 , C07C209/70 , C07C211/61 , C07C2603/66 , C07C23/10
摘要： The present invention relates to a novel a process for the preparation of the compound of the general formula (I), wherein R1 and R2 are independently H or C1-6 alkyl, which comprises treating with a reducing agent either a compound of the general formula (II), wherein R1 and R2 have the meanings given for the compound of the formula (I), R3 is H or C1-4alkyl and Ph is phenyl, or a compound of the general formula (III), wherein R1, R2, R3 and Ph have the meanings given for the compound of the formula (II), the reducing agent being effective to cleave the benzyl moiety Ph-CH(R3)— from the benzylamino moiety PhCH(R3)NH— in the compound of the formula (II) or in the compound of the formula (III) to leave an amino group and, in addition, in the case of the compound of the formula (III), to reduce both the 2,3-double bond and the double bond joining the R1R2C— moiety to the 9-position of the benzonorbornene ring to single bonds. It also relates to processes for the preparation of the compounds (II) and (III) and their precursors and to the compounds (II) and (III) themselves and certain of their precursors, which are novel compounds. The compounds (I) are useful for the preparation of various fungicidal heterocyclyl-carboxylic acid benzonorbornen-5-yl-amides.
摘要翻译：本发明涉及一种制备通式（I）化合物的方法，其中R 1和R 2独立地为H或C 1-6烷基，其包括用还原剂处理通式（II）化合物，其中R1和R2具有式（I）化合物所给出的含义，R 3是H或C 1-4烷基，Ph是苯基，或通式（III）的化合物，其中R1，R2， R3和Ph具有式（II）化合物所给出的含义，还原剂有效地从式（II）化合物中的苄基氨基部分PhCH（R3）NH-切割苄基部分Ph-CH（R3）（II）化合物或式（III）化合物中，以留下氨基，另外，在式（III）化合物的情况下，为了还原2,3-双键和双键将R1R2C-部分连接到苯并降冰片烯环的9位到单键。它还涉及制备化合物（II）和（III）及其前体以及化合物（II）和（III）本身及其某些新型化合物的前体的方法。化合物（I）可用于制备各种杀真菌性杂环基 - 羧酸苯并降冰片烯-5-基 - 酰胺。

6. 发明申请

US20090221856A1 PROCESS FOR THE PREPARATION OF AMINES 有权
标题翻译：制备氨基酸的方法
公开(公告)号：US20090221856A1
公开(公告)日：2009-09-03
申请号：US12096796
申请日：2006-12-11
申请人： Hans Tobler , Harald Walter , Camilla Corsi , Josef Ehrenfreund , Fanny Giordano , Martin Zeller
发明人： Hans Tobler , Harald Walter , Camilla Corsi , Josef Ehrenfreund , Fanny Giordano , Martin Zeller
IPC分类号： C07C211/31
CPC分类号： C07C209/62 , C07B2200/09 , C07C17/23 , C07C17/30 , C07C17/354 , C07C25/22 , C07C25/24 , C07C209/10 , C07C209/70 , C07C211/61 , C07C2603/66 , C07C23/10
摘要： The present invention relates to a novel a process for the preparation of the compound of the general formula (I), wherein R1 and R2 are independently H or C1-6 alkyl, which comprises treating with a reducing agent either a compound of the general formula (II), wherein R1 and R2 have the meanings given for the compound of the formula (I), R3 is H or C1-4alkyl and Ph is phenyl, or a compound of the general formula (III), wherein R1, R2, R3 and Ph have the meanings given for the compound of the formula (II), the reducing agent being effective to cleave the benzyl moiety Ph-CH(R3)— from the benzylamino moiety PhCH(R3)NH— in the compound of the formula (II) or in the compound of the formula (III) to leave an amino group and, in addition, in the case of the compound of the formula (III), to reduce both the 2,3-double bond and the double bond joining the R1R2C— moiety to the 9-position of the benzonorbornene ring to single bonds. It also relates to processes for the preparation of the compounds (II) and (III) and their precursors and to the compounds (II) and (III) themselves and certain of their precursors, which are novel compounds. The compounds (I) are useful for the preparation of various fungicidal heterocyclyl-carboxylic acid benzonorbornen-5-yl-amides.
摘要翻译：本发明涉及一种制备通式（I）化合物的方法，其中R 1和R 2独立地为H或C 1-6烷基，其包括用还原剂处理通式（II）化合物，其中R1和R2具有式（I）化合物所给出的含义，R 3是H或C 1-4烷基，Ph是苯基，或通式（III）的化合物，其中R1，R2， R3和Ph具有式（II）化合物所给出的含义，还原剂有效地从式（II）化合物中的苄基氨基部分PhCH（R3）NH-切割苄基部分Ph-CH（R3）（II）化合物或式（III）化合物中，以留下氨基，另外，在式（III）化合物的情况下，为了还原2,3-双键和双键将R1R2C-部分连接到苯并降冰片烯环的9位到单键。它还涉及制备化合物（II）和（III）及其前体以及化合物（II）和（III）本身及其某些新型化合物的前体的方法。化合物（I）可用于制备各种杀真菌性杂环基 - 羧酸苯并降冰片烯-5-基 - 酰胺。

7. 发明授权

US08536089B2 Fungicidal compositions 有权
标题翻译：杀真菌剂
公开(公告)号：US08536089B2
公开(公告)日：2013-09-17
申请号：US11573277
申请日：2005-08-11
申请人： Harald Walter , Urs Neuenschwander , Ronald Zeun , Josef Ehrenfreund , Hans Tobler , Camilla Corsi , Clemens Lamberth
发明人： Harald Walter , Urs Neuenschwander , Ronald Zeun , Josef Ehrenfreund , Hans Tobler , Camilla Corsi , Clemens Lamberth
IPC分类号： A01N43/56 , A01N43/00 , A01N43/36 , A01N43/40 , A01N43/54 , A01N63/00
CPC分类号： A01N43/56 , A01N43/36 , A01N43/653 , A01N43/707 , A01N43/90 , A01N2300/00
摘要： The invention relates to fungicidal compositions comprising as active ingredient a combination of components A) and B) as defined in the patent claims, to a method of controlling phytopathogenic diseases on crop plants using such a compositions and to a method of protecting natural substances of vegetable and/or animal origin and/or their processed forms using such a composition.
摘要翻译：本发明涉及杀真菌组合物，其包含作为活性成分的组合物A）和B）如专利权利要求中所定义的组合，使用这种组合物控制作物植物病原性疾病的方法和保护植物天然物质的方法和/或动物来源和/或其加工形式。

8. 发明授权

US08207207B2 Heterocyclic a amide derivatives useful as microbiocides 有权
标题翻译：杂环酰胺衍生物可用作杀微生物剂
公开(公告)号：US08207207B2
公开(公告)日：2012-06-26
申请号：US12765942
申请日：2010-04-23
申请人： Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi
发明人： Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi
IPC分类号： A01N43/78 , A01P1/00
CPC分类号： C07C205/06 , A01N43/32 , A01N43/36 , A01N43/40 , A01N43/56 , A01N43/647 , A01N43/76 , A01N43/78 , C07C205/11 , C07C205/12 , C07C205/37 , C07C205/45 , C07C211/61 , C07C2603/66 , C07D207/34 , C07D207/46 , C07D213/89 , C07D231/14 , C07D249/04 , C07D263/34 , C07D277/56 , C07D327/06
摘要： The invention relates to a fungicidally active compound of formula (I): as defined in claim 1; to the preparation of these compounds, to novel intermediates used in the preparation of these compounds, to agrochemical compositions which comprise at least one of the novel compounds as active ingredient, to the preparation of the compositions mentioned and to the use of the active ingredients or compositions in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.
摘要翻译：本发明涉及式（I）的杀真菌活性化合物：如权利要求1所定义; 涉及这些化合物的制备，用于制备这些化合物的新型中间体，包括至少一种新化合物作为活性成分的农用化学组合物，所述组合物的制备以及使用活性成分或用于通过植物病原微生物，优选真菌控制或预防植物感染的农业或园艺成分。

9. 发明授权

US08183416B2 Heterocyclic amide derivatives useful as microbiocides 有权
标题翻译：用作杀微生物剂的杂环酰胺衍生物
公开(公告)号：US08183416B2
公开(公告)日：2012-05-22
申请号：US12765929
申请日：2010-04-23
申请人： Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi
发明人： Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi
IPC分类号： C07C205/06
CPC分类号： C07C205/06 , A01N43/32 , A01N43/36 , A01N43/40 , A01N43/56 , A01N43/647 , A01N43/76 , A01N43/78 , C07C205/11 , C07C205/12 , C07C205/37 , C07C205/45 , C07C211/61 , C07C2603/66 , C07D207/34 , C07D207/46 , C07D213/89 , C07D231/14 , C07D249/04 , C07D263/34 , C07D277/56 , C07D327/06
摘要： The invention relates to a fungicidally active compound of formula (I): where Het is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, the ring being substituted by the groups R6, R7 and R8; R1 is hydrogen, C1-4 alkyl, C1-4 haloalkyl, C1-4alkoxy, C1-4haloalkoxy, CH2C≡CR9, CH2CR10═CHR11, CH═C═CH2 or COR12; R2 and R3 are each, independently, hydrogen, halo, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl or C1-4 haloalkoxy; R4 and R5 are each independently selected from halo, cyano and nitro; or one of R4 and R5 is hydrogen and the other is selected from halo, cyano and nitro; R6, R7 and R8 are each, independently, hydrogen, halo, cyano, nitro, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy(C1-4)alkyl, C1-4haloalkoxy(C1-4)alkyl or C1-4haloalkoxy, provided that at least one of R6, R7 and R8 is not hydrogen; R9, R10 and R11 are each, independently, hydrogen, halo, C1-4 alkyl, C1-4 haloalkyl or C1-4 alkoxy(C1-4)alkyl; and R12 is hydrogen, C1-6 alkyl, C1-6haloalkyl, C1-4 alkoxy(C1-4)alkyl, C1-4 alkylthio(C1-4)-alkyl, C1-4 alkoxy or aryl; to the preparation of these compounds, to novel intermediates used in the preparation of these compounds, to agrochemical compositions which comprise at least one of the novel compounds as active ingredient, to the preparation of the compositions mentioned and to the use of the active ingredients or compositions in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.
摘要翻译：本发明涉及式（I）的杀真菌活性化合物：其中Het是含有一至三个杂原子的5-或6-元杂环，各自独立地选自氧，氮和硫，该环被R6基团取代，R7和R8; R 1是氢，C 1-4烷基，C 1-4卤代烷基，C 1-4烷氧基，C 1-4卤代烷氧基，CH 2C≡CR9，CH 2 CR 10 = CHR 11，CH = C = CH 2或COR 12; R 2和R 3各自独立地为氢，卤素，C 1-4烷基，C 1-4烷氧基，C 1-4卤代烷基或C 1-4卤代烷氧基; R4和R5各自独立地选自卤素，氰基和硝基; 或者R 4和R 5中的一个是氢，另一个选自卤素，氰基和硝基; R 6，R 7和R 8各自独立地为氢，卤素，氰基，硝基，C 1-4烷基，C 1-4卤代烷基，C 1-4烷氧基（C 1-4）烷基，C 1-4卤代烷氧基（C 1-4）烷基或C 1 -4卤代烷氧基，条件是R 6，R 7和R 8中的至少一个不是氢; R 9，R 10和R 11各自独立地为氢，卤素，C 1-4烷基，C 1-4卤代烷基或C 1-4烷氧基（C 1-4）烷基; 并且R 12是氢，C 1-6烷基，C 1-6卤代烷基，C 1-4烷氧基（C 1-4）烷基，C 1-4烷硫基（C 1-4） - 烷基，C 1-4烷氧基或芳基; 涉及这些化合物的制备，用于制备这些化合物的新型中间体，包括至少一种新化合物作为活性成分的农用化学组合物，所述组合物的制备以及使用活性成分或用于通过植物病原微生物，优选真菌控制或预防植物感染的农业或园艺成分。

10. 发明授权

US07820830B2 Process for the production of carboxanilides 有权
标题翻译：生产甲酰苯胺的方法
公开(公告)号：US07820830B2
公开(公告)日：2010-10-26
申请号：US12093619
申请日：2006-11-13
申请人： Harald Walter , Camilla Corsi , Josef Ehrenfreund , Hans Tobler
发明人： Harald Walter , Camilla Corsi , Josef Ehrenfreund , Hans Tobler
IPC分类号： C07D231/14
CPC分类号： C07D231/14
摘要： The present invention relates to a novel process for the preparation of a compound of general formula (I): wherein R1 is H or C1-4 alkyl and R2 is difluoromethyl or trifluoromethyl, which comprises reacting a compound of general formula (II): wherein R1 has the meaning given above and X is chloro or bromo, with a compound of general formula (III): wherein R2 has the meaning given above, in the presence of a base, a palladium catalyst and a ferrocenyl biphoshine ligand of the Josiphos type, the reaction being carried out in an ether solvent at a reflux temperature of at least 100° C.
摘要翻译：本发明涉及一种制备通式（I）化合物的新方法：其中R1是H或C1-4烷基，R2是二氟甲基或三氟甲基，其包括使通式（II）的化合物：其中 R1具有上面给出的含义，X是氯或溴，与通式（III）的化合物：其中R 2具有上面给出的含义，在碱存在下，钯催化剂和Josiphos型的二茂铁基二膦配体，反应在乙醚溶剂中在至少100℃的回流温度下进行。

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