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    PROCESS FOR THE PREPARATION OF PYRAZOLE CARBOXYLIC ACID AMIDES
    3.
    发明申请
    PROCESS FOR THE PREPARATION OF PYRAZOLE CARBOXYLIC ACID AMIDES 审中-公开
    制备吡唑羧酸酰胺的方法

    公开(公告)号：WO2011131543A1

    公开(公告)日：2011-10-27

    申请号：PCT/EP2011/055869

    申请日：2011-04-14

    Applicant: SYNGENTA PARTICIPATIONS AG ,  DUMEUNIER, Raphael ,  TOBLER, Hans

    Inventor： DUMEUNIER, Raphael ,  TOBLER, Hans

    IPC: C07D231/14 ,  C07D303/08 ,  C07D303/36 ,  C07C211/61

    CPC classification number: C07D231/14 ,  C07D303/08 ,  C07D303/36

    Abstract: 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 riphenylphosphane/bromotrichloromethane to the compound of formula I.

    Abstract translation: 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。

    PROCESS FOR THE STEREOSELECTIVE PREPARATION OF A PYRAZOLE-CARBOXAMIDE
    5.
    发明申请
    PROCESS FOR THE STEREOSELECTIVE PREPARATION OF A PYRAZOLE-CARBOXAMIDE 审中-公开
    吡唑酰胺的立体选择性制备方法

    公开(公告)号：WO2014206855A1

    公开(公告)日：2014-12-31

    申请号：PCT/EP2014/062936

    申请日：2014-06-19

    Applicant: SYNGENTA PARTICIPATIONS AG

    Inventor： DUMEUNIER, Raphael ,  KESSABI, Jilali ,  WENDEBORN, Sebastian Volker ,  NUSSBAUMER, Hannes

    IPC: C07D231/14 ,  C07C239/00

    CPC classification number: C07D231/14 ,  C07C239/20

    Abstract: The present invention relates to a process for the enantioselective preparation of the compound of formula (lb), which process comprises a) reducing the (E)- or (Z)-form of a compound of formula (II), with an enantioselective reagent to a compound of formula (IlIa), and b) acylating the compound of formula (IlIa) with the compound of formula (IV), or c) coupling the compound of formula (IV) with the compound of formula (II), to give a compound of formula (V)and d) reducing compound of formula (V) in the presence of hydrogen, a catalyst and a chiral ligand, to the compound of formula (lb).

    Abstract translation: 本发明涉及式（Ib）化合物的对映选择性制备方法，该方法包括a）用对映选择性试剂还原式（II）化合物的（E） - 或（Z） 与式（Ⅺa）化合物反应，和b）用式（Ⅳ）化合物酰化式（Ⅺa）化合物，或c）将式（Ⅳ）化合物与式（Ⅳ）化合物偶联至 在式（Ⅴ）化合物和式（Ⅴ）化合物的存在下，在氢气，催化剂和手性配体的存在下，得到式（Ⅴ）化合物和d）还原式（Ⅴ）化合物。

    NOVEL IMIDAZOLE DERIVATIVES HAVING MICROBIOCIDAL ACTIVITY
    7.
    发明申请
    NOVEL IMIDAZOLE DERIVATIVES HAVING MICROBIOCIDAL ACTIVITY 审中-公开
    具有微生物活性的新咪唑烷衍生物

    公开(公告)号：WO2009127615A1

    公开(公告)日：2009-10-22

    申请号：PCT/EP2009/054389

    申请日：2009-04-14

    Applicant: SYNGENTA PARTICIPATIONS AG ,  DUMEUNIER, Raphael ,  LAMBERTH, Clemens ,  TRAH, Stephan

    Inventor： DUMEUNIER, Raphael ,  LAMBERTH, Clemens ,  TRAH, Stephan

    IPC: C07D233/60 ,  C07D233/68 ,  C07D403/12 ,  A01N43/50 ,  A61K31/4489 ,  A61P35/00

    CPC classification number: C07D233/68 ,  C07D233/60 ,  C07D403/12

    Abstract: The present invention relates to novel imidazole derivatives of formula I as active ingredients which have microbiocidal activity, in particular fungicidal activity wherein (I) wherein R 1 is halogen, C 1 -C 4 alkyl or C 1 -C 4 haloalkyl, R 2 is an optionally substituted aryl, R 3 is halogen or OR 7 , R 4 and R 5 are, independently of each other, hydrogen, halogen or OR 7 , R 6 is halogen or C 1 -C 4 alkyl, and R 7 is hydrogen, C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, C 3 -C 10 cycloalkylalkyl, C 1 -C 6 haloalkyl, C 2 -C 6 alkenyl, C 2 -C 6 haloalkenyl, C3-C7 cycloalkenyl, C 2 -C 6 alkynyl, C 2 -C 6 haloalkynyl, C 2 -C 6 alkyloxyalkyl, C 3 -C 8 dialkylaminoalkyl, C 4 -C 10 cycloalkylaminoalkyl or C4-C10 heterocyclylalkyl, or an agrochemically usable salt form thereof, provided that when R 3 is halogen, at least one of R 4 or R 5 is OR 7 , or when R 3 is OR7, at least one of R 4 or R 5 is OR 7 or halogen

    Abstract translation: 本发明涉及式I的新型咪唑衍生物，其具有杀微生物活性，特别是杀真菌活性的活性成分，其中（I）其中R1是卤素，C1-C4烷基或C1-C4卤代烷基，R2是任选取代的芳基，R3是卤素 或OR7，R4和R5彼此独立地为氢，卤素或OR7，R6为卤素或C1-C4烷基，R7为氢，C1-C6烷基，C3-C7环烷基，C3-C10环烷基烷基，C1- C 6卤代烷基，C 2 -C 6烯基，C 2 -C 6卤代烯基，C 3 -C 7环烯基，C 2 -C 6炔基，C 2 -C 6卤代炔基，C 2 -C 6烷氧基烷基，C 3 -C 8二烷基氨基烷基，C 4 -C 10环烷基氨基烷基或C 4 -C 10杂环基烷基， 条件是当R 3为卤素时，R 4或R 5中的至少一个为OR 7，或者当R 3为OR 7时，R 4或R 5中的至少一个为OR 7或卤素

    NOVEL PYRAZOLE DERIVATIVES
    8.
    发明申请
    NOVEL PYRAZOLE DERIVATIVES 审中-公开
    新型吡咯衍生物

    公开(公告)号：WO2009127612A1

    公开(公告)日：2009-10-22

    申请号：PCT/EP2009/054386

    申请日：2009-04-14

    Applicant: SYNGENTA PARTICIPATIONS AG ,  DUMEUNIER, Raphael ,  LAMBERTH, Clemens ,  TRAH, Stephan

    Inventor： DUMEUNIER, Raphael ,  LAMBERTH, Clemens ,  TRAH, Stephan

    IPC: C07D231/16 ,  A61K31/33 ,  A61P35/00 ,  A01N43/00

    CPC classification number: C07D231/16 ,  A01N43/56

    Abstract: The present invention relates tonovel pyrazolederivatives of Formula (I) as active ingredients which have microbiocidal activity, in particular fungicidal activity: wherein R 1 is C 1 -C 4 alkyl or C 1 -C haloalkyl; R 2 is an optionally substituted aryl or heteroaryl; R 3 is halogen; R 4 is hydrogen, halogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, cyano or OR 6 ; R 5 is hydrogen, halogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, cyano or OR 6 ; R 6 is hydrogen, C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, C 3 -C 10 alkylcycloalkyl, C 1 -C 6 haloalkyl, C 2 -C 6 alkenyl, C 2 -C haloalkenyl, C 3 -C 7 cycloalkenyl, C 2 -C 6 alkynyl, C 2 -C 6 haloalkynyl, C 2 -C 6 alkyloxyalkyl; R 7 is halogen or OR 6 ; X is N or C-R 4 ; or an agrochemically usablesalt form thereof.

    Abstract translation: 本发明涉及具有杀微生物活性，特别是杀真菌活性的作为活性成分的式（I）的次级吡唑衍生物，其中R1是C1-C4烷基或C1-C卤代烷基; R2是任选取代的芳基或杂芳基; R3是卤素; R4是氢，卤素，C1-C4烷基，C1-C4卤代烷基，氰基或OR6; R5是氢，卤素，C1-C4烷基，C1-C4卤代烷基，氰基或OR6; R6是氢，C1-C6烷基，C3-C7环烷基，C3-C10烷基环烷基，C1-C6卤代烷基，C2-C6烯基，C2-C卤代烯基，C3-C7环烯基，C2-C6炔基，C2-C6卤代炔基，C2 -C 6烷氧基烷基; R7为卤素或OR6; X为N或C-R4; 或其农业化学用途形式。

    DIAZA-INDOLE DERIVATIVES AND THEIR USE AS FUNGICIDES
    9.
    发明申请
    DIAZA-INDOLE DERIVATIVES AND THEIR USE AS FUNGICIDES 审中-公开
    DIAZA-INDOLE DORIVATIVES及其作为FUNGICIDES的用途

    公开(公告)号：WO2010046215A2

    公开(公告)日：2010-04-29

    申请号：PCT/EP2009/062673

    申请日：2009-09-30

    Applicant: SYNGENTA PARTICIPATIONS AG ,  SELLES, Patrice ,  SRINIVAS, Nityakalyani ,  DUMEUNIER, Raphael ,  CEDERBAUM, Frederik ,  UMARYE, Jayant

    Inventor： SELLES, Patrice ,  SRINIVAS, Nityakalyani ,  DUMEUNIER, Raphael ,  CEDERBAUM, Frederik ,  UMARYE, Jayant

    CPC classification number: A01N43/90 ,  C07D471/04 ,  C07D487/04

    Abstract: The present invention relates to novel compounds of the formula (I) in which any one of G 1 , G 2 and G 3 is N and the other two of G 1 , G 2 and G 3 are CR 8 , CR 1 or CR 2 , such that when G 1 is not N, G 1 is CR 8 ; when G 2 is not N, G 2 is CR 1 ; when G 3 is not N, G 3 is CR 2 ; and X 1 , X 2 , R 1 , R 2 , R 3 , R 4 , R 6 , R 7 , and R 8 are as defined in the claims. In particular, the invention relates to use of these compounds in methods for the control and/or prevention of fungal infection in plants. The invention also relates to compositions containing these compounds as well as methods for preparing these compounds.

    Abstract translation: 本发明涉及式（I）的新化合物，其中，G1，G2和G3中的任一个为N，而G1，G2和G3中的任一个为CR8，CR1或CR2，使得当G1不为N时， G1是CR8; 当G2不是N时，G2是CR1; 当G3不为N时，G3为CR2; 并且X 1，X 2，R 1，R 2，R 3，R 4，R 6，R 7和R 8如权利要求中所定义。 特别地，本发明涉及这些化合物在控制和/或预防植物真菌感染的方法中的用途。 本发明还涉及含有这些化合物的组合物以及制备这些化合物的方法。

    PYRIDAZINE FUNGICIDES
    10.
    发明申请
    PYRIDAZINE FUNGICIDES 审中-公开
    吡咯烷类杀真菌剂

    公开(公告)号：WO2009090039A1

    公开(公告)日：2009-07-23

    申请号：PCT/EP2009/000166

    申请日：2009-01-14

    Applicant: SYNGENTA PARTICIPATIONS AG ,  TRAH, Stephan ,  LAMBERTH, Clemens ,  DUMEUNIER, Raphael ,  WENDEBORN, Sebastian, Volker

    Inventor： TRAH, Stephan ,  LAMBERTH, Clemens ,  DUMEUNIER, Raphael ,  WENDEBORN, Sebastian, Volker

    IPC: C07D401/04 ,  A01N43/58 ,  A61P35/00

    CPC classification number: C07D401/04

    Abstract: The present invention relates to novel pyridazine derivatives of formula (I) as active ingredients which have microbiocidal activity, in particular fungicidal activity: wherein R 1 is methyl, ethyl or isopropyl; R 2 is chloro, fluoro, hydroxy or C 1 -C 2 alkoxy; R 3 is H, chloro, fluoro, methoxy or C 1 -C 3 alkyl; R 4 is chloro, fluoro or bromo; and R 5 is H, fluoro or methoxy; or an agrochemically usable salt form thereof; with the proviso that when R 1 is methyl, R 2 is chloro and R 3 is H, then R 4 or R 5 is different from fluoro.

    Abstract translation: 本发明涉及式（I）的新的哒嗪衍生物作为具有杀微生物活性的活性成分，特别是杀真菌活性：其中R1是甲基，乙基或异丙基; R2是氯，氟，羟基或C1-C2烷氧基; R3是H，氯，氟，甲氧基或C1-C3烷基; R4是氯，氟或溴; R5为H，氟或甲氧基; 或其农业化学可用的盐形式; 条件是当R 1为甲基时，R 2为氯且R 3为H，则R 4或R 5不同于氟。

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