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    PROCESS FOR THE PREPARATION OF PYRAZOLE CARBOXYLIC ACID AMIDES
    1.
    发明申请
    PROCESS FOR THE PREPARATION OF PYRAZOLE CARBOXYLIC ACID AMIDES 有权
    制备吡唑羧酸酰胺的方法

    公开(公告)号：US20130041161A1

    公开(公告)日：2013-02-14

    申请号：US13642512

    申请日：2011-04-14

    申请人： Raphael Dumeunier ,  Hans Tobler

    发明人： Raphael Dumeunier ,  Hans Tobler

    IPC分类号： C07D231/14 ,  C07C215/70 ,  C07D303/36

    CPC分类号： C07D231/14 ,  C07D303/08 ,  C07D303/36

    摘要： The invention relates to a process for the preparation of formula (I), which process comprises a) reacting the compound (II), with cyclopentadiene to (III); b) reacting this compound in the presence of an oxidant to the compound of formula (IV); c) hydrogenating this compound in the presence of a metal catalyst and an inert solvent under hydrogen atmosphere to the compound of formula (V); d) reacting this compound in the presence of a Brönsted acid followed by a reducing agent to the compound of formula (VI); e) reacting VI with a compound (VII), in the presence of a base to a compound of formula (VIII); f) converting the compound of formula VIII in the presence of an oxidising agent to the compound of formula (IX); and g) reacting the compound of formula IX in the presence of triphenylphosphane/carbon tetrachloride or triphenylphosphane/bromotrichloromethane to the compound of formula I.

    摘要翻译： 本发明涉及制备式（I）的方法，该方法包括：a）使化合物（II）与环戊二烯反应至（III）; b）在氧化剂存在下使该化合物与式（Ⅳ）化合物反应; c）在金属催化剂和惰性溶剂的存在下，在氢气氛下将该化合物氢化成式（V）化合物; d）在布朗斯台德酸的存在下将该化合物与式（VI）化合物的还原剂反应; e）使VI与化合物（VII）在碱的存在下与式（VIII）的化合物反应; f）将式VIII化合物在氧化剂存在下转化为式（Ⅸ）化合物; 和g）在三苯基膦/四氯化碳或三苯基膦/溴三氯甲烷存在下将式IX化合物与式I化合物反应。

    Process for the preparation of pyrazole carboxylic acid amides
    2.
    发明授权
    Process for the preparation of pyrazole carboxylic acid amides 有权
    制备吡唑羧酸酰胺的方法

    公开(公告)号：US08450499B2

    公开(公告)日：2013-05-28

    申请号：US13642512

    申请日：2011-04-14

    申请人： Raphael Dumeunier ,  Hans Tobler

    发明人： Raphael Dumeunier ,  Hans Tobler

    IPC分类号： C07D231/10 ,  C07D303/02 ,  C07C211/43

    CPC分类号： C07D231/14 ,  C07D303/08 ,  C07D303/36

    摘要： The invention relates to a process for the preparation of formula (I), which process comprises a) reacting the compound (II), with cyclopentadiene to (III); b) reacting this compound in the presence of an oxidant to the compound of formula (IV); c) hydrogenating this compound in the presence of a metal catalyst and an inert solvent under hydrogen atmosphere to the compound of formula (V); d) reacting this compound in the presence of a Brönsted acid followed by a reducing agent to the compound of formula (VI); e) reacting VI with a compound (VII), in the presence of a base to a compound of formula (VIII); f) converting the compound of formula VIII in the presence of an oxidizing agent to the compound of formula (IX); and g) reacting the compound of formula IX in the presence of triphenylphosphane/carbon tetrachloride or riphenylphosphane/bromotrichloromethane to the compound of formula I.

    摘要翻译： 本发明涉及制备式（I）的方法，该方法包括：a）使化合物（II）与环戊二烯反应至（III）; b）在氧化剂存在下使该化合物与式（Ⅳ）化合物反应; c）在金属催化剂和惰性溶剂的存在下，在氢气氛下将该化合物氢化成式（V）化合物; d）在布朗斯台德酸的存在下将该化合物与式（VI）化合物的还原剂反应; e）使VI与化合物（VII）在碱的存在下与式（VIII）的化合物反应; f）将式VIII化合物在氧化剂存在下转化为式（Ⅸ）化合物; 和g）在三苯基膦/四氯化碳或联苯基膦/溴三氯甲烷存在下将式IX化合物与式I化合物反应。

    Heterocyclic amide derivatives useful as microbiocides
    5.
    发明授权
    Heterocyclic amide derivatives useful as microbiocides 有权
    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。

    Process for the production of carboxanilides
    7.
    发明授权
    Process for the production of carboxanilides 有权
    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。

    HETEROCYCLIC AMIDE DERIVATIVES USEFUL AS MICROBIOCIDES
    8.
    发明申请
    HETEROCYCLIC AMIDE DERIVATIVES USEFUL AS MICROBIOCIDES 有权
    杂环酰胺衍生物作为微生物有用

    公开(公告)号：US20100204482A1

    公开(公告)日：2010-08-12

    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 ,  C07D277/56

    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各自独立地是氢，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R4和R5之一是氢，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。

    PROCESS FOR THE PREPARATION OF AMINES
    9.
    发明申请
    PROCESS FOR THE PREPARATION OF AMINES 审中-公开
    制备氨基酸的方法

    公开(公告)号：US20100145100A1

    公开(公告)日：2010-06-10

    申请号：US12443082

    申请日：2007-09-26

    申请人： Harald Walter ,  Hans Tobler ,  Fanny Giordano ,  Martin Zeller

    发明人： Harald Walter ,  Hans Tobler ,  Fanny Giordano ,  Martin Zeller

    IPC分类号： C07C209/36

    CPC分类号： C07C209/36 ,  C07C2603/66 ,  C07C211/61

    摘要： The present invention relates to a process for the preparation of syn-enriched 5-amino-9-isopropyl-benzonorbomene in which the ratio of compounds of formula (Ia(syn)) to compounds of formula (Ib(anti)) is from 70:30 to 99:1, which process comprises reacting a compound of formula (Il) in a pressure vessel with hydrogen in the presence of a palladium catalyst and a solvent, at a pressure of at least 2 bar and a temperature of from 00 C to 45° C., to form syn-enriched 5-amino-9-isopropyl-benzonorbomene.

    摘要翻译： 本发明涉及制备合成富集的5-氨基-9-异丙基 - 苯并异戊烯的方法，其中式（Ia（顺式））化合物与式（Ib（反））化合物的比例为70 ：30至99:1，该方法包括在钯催化剂和溶剂存在下，将压力容器中的式（II）化合物与氢气在至少2巴的压力和0℃的温度下反应 至45℃，以形成合成富集的5-氨基-9-异丙基 - 苯并异戊烯。

    Microbiocides
    10.
    发明授权
    Microbiocides 失效
    杀微生物剂

    公开(公告)号：US07723371B2

    公开(公告)日：2010-05-25

    申请号：US12092338

    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： A01N43/56

    CPC分类号： A01N43/36 ,  A01N43/40 ,  A01N43/56 ,  A01N43/78 ,  A01N43/84 ,  C07C211/45 ,  C07C211/52 ,  C07C2601/02 ,  C07C2601/04 ,  C07D207/34 ,  C07D213/82 ,  C07D231/14 ,  C07D249/04 ,  C07D277/56 ,  C07D327/06

    摘要： The invention relates to a fungicidally active compound of the general 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 R3, R4 and R5; R1 and R2 are independently H, halo, C1-4 alkyl or C1-4 haloalkyl; and R3, R4 and R5 are each, independently, H, halo, C1-4 alkyl, C1-4 haloalkyl or C1-4 haloalkoxy, provided that at least one of R3, R4 and R5 is not H; to the preparation of these compounds, to novel intermediates used in their preparation, to agrochemical compositions which comprise at least one of the novel compounds as an active ingredient, to the preparation of the compositions and to the use of the active ingredients or compositions in agriculture or horticulture for controlling or preventing infestations of plants by phytopathogenic microorganisms, especially fungi.

    摘要翻译： 本发明涉及通式（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，所述环被 基团R3，R4和R5; R 1和R 2独立地为H，卤素，C 1-4烷基或C 1-4卤代烷基; 并且R 3，R 4和R 5各自独立地为H，卤素，C 1-4烷基，C 1-4卤代烷基或C 1-4卤代烷氧基，条件是R 3，R 4和R 5中的至少一个不为H; 涉及这些化合物的制备，其制备中使用的新型中间体，包含至少一种新化合物作为活性成分的农用化学组合物，用于制备组合物以及在农业中使用活性成分或组合物 或园艺用于通过植物病原微生物，特别是真菌控制或预防植物侵染。