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公开(公告)号：US20130035496A1
公开(公告)日：2013-02-07
申请号：US13642406
申请日：2011-04-14
IPC分类号： C07D231/14 , C07C35/37 , C07C25/18 , C07D303/10
CPC分类号： C07D231/14 , C07C17/23 , C07C17/30 , C07C25/24 , C07C29/132 , C07C35/52 , C07C45/29 , C07C209/10 , C07C2603/66 , C07D303/17 , C07C49/697 , C07C23/10 , C07C25/22 , C07C211/61
摘要： The invention relates to a process for the preparation of the compound of formula (I), which process comprises a) reacting a compound of formula (II), wherein X is chloro or bromo, with an organometallic species in an inert atmosphere to a halobenzyne of formula (X), reacting the halobenzyne of formula X so formed with cyclopentadiene to (III), b) reacting III in the presence of an inert solvent with an oxidant to (IV), c) reacing IV in the presence of a Lewis acid and a hydride source to (V), d) reacting V in the presence of an oxidizing agent, a base and an inert solvent to (VI), e) converting VI in the presence of a phosphane and CCL4 or CHCl3 to (VII), and either f1) reacting VII with NH3 in the presence of a catalyst to the compound of formula (VIII); and g) reacting VIII in the presence of a base with a compound of formula (IX), to the compound of formula (I); or f2) reacting the compound of formula (VII), in the presence of a solvent, a base, a copper catalyst and at least one ligand with the compound of formula (IXa), to the compound of formula (I).
摘要翻译： 本发明涉及一种制备式（I）化合物的方法，该方法包括：a）使惰性气氛下的有机金属物质使式（II）化合物（其中X为氯或溴）与卤代苯 使式（X）所示的卤代苯与环戊二烯反应，（b）使惰性溶剂与惰性溶剂的存在下的III反应与式（Ⅳ）反应：c）在Lewis 酸和氢化物源至（V），d）使V在氧化剂，碱和惰性溶剂的存在下与（VI）反应，e）将VI在磷烷和CCL 4或CHCl 3存在下转化为（VII ），并且f1）使VII与NH 3在催化剂存在下与式（VIII）化合物反应; 和g）在碱存在下使VIII与式（IX）化合物反应，得到式（I）化合物; 或者f2）使式（Ⅶ）化合物在溶剂存在下，碱，铜催化剂和至少一种配体与式（Ⅸa）化合物反应，得到式（I）化合物。
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公开(公告)号：US08519152B2
公开(公告)日：2013-08-27
申请号：US13642406
申请日：2011-04-14
IPC分类号： C07D231/10 , C07D303/02 , C07C33/00
CPC分类号： C07D231/14 , C07C17/23 , C07C17/30 , C07C25/24 , C07C29/132 , C07C35/52 , C07C45/29 , C07C209/10 , C07C2603/66 , C07D303/17 , C07C49/697 , C07C23/10 , C07C25/22 , C07C211/61
摘要： The invention relates to a process for the preparation of the compound of formula (I), which process comprises a) reacting a compound of formula (II), wherein X is chloro or bromo, with an organometallic species in an inert atmosphere to a halobenzyne of formula (X), reacting the halobenzyne of formula X so formed with cyclopentadiene to (III), b) reacting III in the presence of an inert solvent with an oxidant to (IV), c) reacting IV in the presence of a Lewis acid and a hydride source to (V), d) reacting V in the presence of an oxidizing agent, a base and an inert solvent to (VI), e) converting VI in the presence of a phosphane and CCl4 or CHCl3 to (VII), and either f1) reacting VII with NH3 in the presence of a catalyst to the compound of formula (VIII); and g) reacting VIII in the presence of a base with a compound of formula (IX), to the compound of formula (I); or f2) reacting the compound of formula (VII), in the presence of a solvent, a base, a copper catalyst and at least one ligand with the compound of formula (IXa), to the compound of formula (I).
摘要翻译： 本发明涉及一种制备式（I）化合物的方法，该方法包括：a）使惰性气氛下的有机金属物质使式（II）化合物（其中X为氯或溴）与卤代苯 使式（X）所示的卤代苯与环戊二烯反应，得到（III），b）使III在惰性溶剂存在下与氧化剂反应，得到（Ⅳ），c）使IV在Lewis 酸和氢化物源至（V），d）使V在氧化剂，碱和惰性溶剂的存在下与（VI）反应，e）在磷烷和CCl 4或CHCl 3存在下将VI转化为（VII ），并且f1）使VII与NH 3在催化剂存在下与式（VIII）化合物反应; 和g）在碱存在下使VIII与式（IX）化合物反应，得到式（I）化合物; 或者f2）使式（Ⅶ）化合物在溶剂存在下，碱，铜催化剂和至少一种配体与式（Ⅸa）化合物反应，得到式（I）化合物。
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3.发明申请PYRIDAZINE DERIVATIVES USEFUL AS FUNGICIDES AND FOR THE TREATMENT OF CANCER 审中-公开用作杀真菌剂和治疗癌症的吡咯烷酮衍生物公开(公告)号：US20100273804A1
公开(公告)日：2010-10-28
申请号：US12809604
申请日：2008-12-19
IPC分类号： A61K31/501 , A01N43/58 , C07D403/04 , C07D237/08 , A01P3/00 , A61K31/50 , A61P35/00
CPC分类号： C07D237/12 , A01N43/58 , C07D237/14
摘要： The present invention relates to novel pyridazine derivatives of formula (I) as active ingredients which have microbiocidal activity, in particular fungicidal activity: formula (I) wherein R1 is C1-C6alkyl, C1-C6haloalkyl or C3-C6cycloalkyl; R2 is hydrogen or an optionally substituted alkyl, aryl or heteroaryl; R3 is hydrogen, C1-C6alkyl or C1-C6haloalkyl; R4 is hydrogen, C1-C6alkyl or C1-C6haloalkyl; or R3 and R4 together can be part of a carbocyclic or heterocyclic 3- to 8-membered ring; R5 is optionally substituted aryl or heteroaryl; and R6 is hydroxy, halogen, C1-C6alkoxy, C1-C6haloalkoxy, C1-C6alkylthio or C1-C6haloalkylthio; or an agrochemically usable salt form thereof.
摘要翻译： 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）的新哒嗪衍生物：式（I）其中R 1是C 1 -C 6烷基，C 1 -C 6卤代烷基或C 3 -C 6环烷基; R 2是氢或任选取代的烷基，芳基或杂芳基; R3是氢，C1-C6烷基或C1-C6卤代烷基; R4是氢，C1-C6烷基或C1-C6卤代烷基; 或者R 3和R 4一起可以是碳环或杂环的3至8元环的一部分; R5是任选取代的芳基或杂芳基; R 6为羟基，卤素，C 1 -C 6烷氧基，C 1 -C 6卤代烷氧基，C 1 -C 6烷硫基或C 1 -C 6卤代烷硫基; 或其农业化学上可用的盐形式。
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公开(公告)号：US20110311649A1
公开(公告)日：2011-12-22
申请号：US12739852
申请日：2008-10-24
IPC分类号： A01N43/40 , C07D401/14 , A01N43/42 , A01N57/00 , A01N43/54 , A01N43/84 , A01N59/20 , C07D401/04 , A01P3/00
CPC分类号： C07D233/61 , C07D233/68 , C07D401/04 , C07D401/14 , C07D409/04 , C07D409/14
摘要： The present invention relates to novel imidazole derivatives of formula (I) as active ingredients which have microbiocidal activity, in particular fungicidal activity: wherein R1 is halogen, C1-C4alkyl or C1-C4haloalkyl; R2 is an optionally substituted aryl or heteroaryl; R3 is halogen; R4 is hydrogen, halogen, C1-C4alkyl, C1-C4haloalkyl, hydroxyl, C1-C4alkoxy, OR6, C1-C4haloalkoxy or cyano; R5 is halogen; R6 is hydrogen, C3-C7 cycloalkyl, C3-C10 alkylcycloalkyl, C1-C6 haloalkyl, C2-C6 alkenyl, C2-C6 haloalkenyl, C3-C7 cycloalkenyl, C2-C6 alkynyl, C2-C6 haloalkynyl or C2-C6 alkyloxyalkyl; X is N or C(R); and R is hydrogen, halogen, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy or cyano; or an agrochemically usable salt form thereof; provided that when X is C(R), R2 cannot be an optionally substituted aryl.
摘要翻译： 本发明涉及式（I）的新咪唑衍生物作为具有杀微生物活性，特别是杀真菌活性的活性成分：其中R1是卤素，C1-C4烷基或C1-C4卤代烷基; R2是任选取代的芳基或杂芳基; R3是卤素; R4是氢，卤素，C1-C4烷基，C1-C4卤代烷基，羟基，C1-C4烷氧基，OR6，C1-C4卤代烷氧基或氰基; R5是卤素; R6是氢，C3-C7环烷基，C3-C10烷基环烷基，C1-C6卤代烷基，C2-C6烯基，C2-C6卤代烯基，C3-C7环烯基，C2-C6炔基，C2-C6卤代炔基或C2-C6烷氧基烷基; X是N或C（R）; 且R为氢，卤素，C 1 -C 4烷基，C 1 -C 4卤代烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷氧基或氰基; 或其农业化学可用的盐形式; 条件是当X是C（R）时，R 2不能是任选取代的芳基。
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公开(公告)号：US20110142802A1
公开(公告)日：2011-06-16
申请号：US12863372
申请日：2009-01-14
申请人： Jeremy R. Godwin , Stephan Trah , Clemens Lamberth , Raphael Dumeunier , Valeria Grasso , Sebastian Volker Wendeborn
发明人： Jeremy R. Godwin , Stephan Trah , Clemens Lamberth , Raphael Dumeunier , Valeria Grasso , Sebastian Volker Wendeborn
IPC分类号： A01N63/04 , A01N59/26 , A01N59/20 , A01N59/18 , A01N59/16 , A01N59/00 , A01N65/26 , A01N65/08 , A01N43/16 , A01N57/20 , A01N37/18 , A01N43/62 , A01N43/88 , A01N43/58 , A01N43/90 , A01P3/00
CPC分类号： A01N43/58 , A01N37/34 , A01N43/54 , A01N43/653 , A01N47/14 , A01N51/00 , A01N2300/00
摘要： A fungicidal composition suitable for control of disease caused by phytopathogens comprising (A) a compound of formula (I), wherein R1 is methyl, ethyl or isopropyl; R2 is 2-chloro-6-fluoro-phenyl, 2,4,6-trifluorophenyl or 2,6-difluoro-4-methoxy-phenyl; R3 is chloro, fluoro or methoxy; and (B) a compound selected, for example, from the group consisting of (B1) a strobilurin fungicide, (B2) an azole fungicide, (B3) a morpholine fungicide, and (B4) an anilinopyrimidine fungicide.
摘要翻译： 一种适于控制由植物病原体引起的疾病的杀真菌组合物，其包含（A）式（I）化合物，其中R 1为甲基，乙基或异丙基; R2是2-氯-6-氟 - 苯基，2,4,6-三氟苯基或2,6-二氟-4-甲氧基 - 苯基; R3是氯，氟或甲氧基; 和（B）选自例如（B1）嗜球果伞素杀真菌剂，（B2）唑类杀真菌剂，（B3）吗啉杀真菌剂和（B4）苯胺基嘧啶杀真菌剂的组合的化合物。
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公开(公告)号：US20110112108A1
公开(公告)日：2011-05-12
申请号：US12863377
申请日：2009-01-14
IPC分类号： A61K31/501 , C07D401/04 , A01N43/48 , A61P35/00 , A01P3/00
CPC分类号： C07D401/04
摘要： The present invention relates to novel pyridazine derivatives of formula (I) as active ingredients which have microbiocidal activity, in particular fungicidal activity: wherein R1 is methyl, ethyl or isopropyl; R2 is chloro, fluoro, hydroxy or C1-C2alkoxy; R3 is H, chloro, fluoro, methoxy or C1-C3alkyl; R4 is chloro, fluoro or bromo; and R3 is H, fluoro or methoxy; or an agrochemically usable salt form thereof; with the proviso that when R1 is methyl, R2 is chloro and R3 is H, then R4 or R5 is different from fluoro.
摘要翻译： 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; 且R 3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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公开(公告)号：US08410026B2
公开(公告)日：2013-04-02
申请号：US12863377
申请日：2009-01-14
IPC分类号： A01N43/58 , A61K31/50 , C07D237/00
CPC分类号： C07D401/04
摘要： The present invention relates to novel pyridazine derivatives of formula (I) as active ingredients which have microbiocidal activity, in particular fungicidal activity: wherein R1 is methyl, ethyl or isopropyl; R2 is chloro, fluoro, hydroxy or C1-C2alkoxy; R3 is H, chloro, fluoro, methoxy or C1-C3alkyl; R4 is chloro, fluoro or bromo; and R5 is H, fluoro or methoxy; or an agrochemically usable salt form thereof; with the proviso that when R1 is methyl, R2 is chloro and R3 is H, then R4 or R5 is different from fluoro.
摘要翻译： 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; R 2是氯，氟，羟基或C 1 -C 2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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公开(公告)号：US20120010195A1
公开(公告)日：2012-01-12
申请号：US13256074
申请日：2010-02-08
IPC分类号： A01N43/46 , A01P3/00 , C07D403/04
CPC分类号： C07D233/88
摘要： The present invention relates to novel imidazole derivatives of formula (I) having microbiocidal, in particular fungicidal, activity, to processes for their preparation and intermediates used in their preparation, to agrochemical compositions comprising them and to the use in agriculture or horticulture for controlling or preventing infestation of plants, harvested food crops, seeds or non-living materials by phytopathogenic microorganisms, preferably fungi.
摘要翻译： 本发明涉及式（I）的新型咪唑衍生物，其具有杀微生物，特别是杀真菌活性，其制备方法和用于其制备的中间体，包含它们的农用化学组合物以及在农业或园艺中用于控制或 通过植物病原微生物，优选真菌预防植物，收获的食物作物，种子或非生物材料的侵染。
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公开(公告)号：US20110224252A1
公开(公告)日：2011-09-15
申请号：US12739863
申请日：2008-10-24
IPC分类号： A01N43/42 , C07D233/68 , A01N43/50 , C07D401/04 , A01N43/40 , C07D409/04 , C07D401/02 , A01P3/00
CPC分类号： C07D401/04 , A01N43/50 , C07D233/28 , C07D401/14 , C07D409/14
摘要： The present invention relates to novel imidazole derivatives of formula (I) as active ingredients which have microbiocidal activity, in particular fungicidal activity: wherein R1 is halogen, C1-C4alkyl or C1-C4haloalkyl; R2 is an optionally substituted aryl or heteroaryl; R3 is halogen; R4 is hydrogen, halogen, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy or cyano; R5 is halogen; X is N or C(R); and R is hydrogen, halogen, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy or cyano; or an agrochemically usable salt form thereof; provided that when X is C(R), R2 cannot be an optionally substituted aryl.
摘要翻译： 本发明涉及式（I）的新咪唑衍生物作为具有杀微生物活性，特别是杀真菌活性的活性成分：其中R1是卤素，C1-C4烷基或C1-C4卤代烷基; R2是任选取代的芳基或杂芳基; R3是卤素; R4是氢，卤素，C1-C4烷基，C1-C4卤代烷基，C1-C4烷氧基，C1-C4卤代烷氧基或氰基; R5是卤素; X是N或C（R）; 且R为氢，卤素，C 1 -C 4烷基，C 1 -C 4卤代烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷氧基或氰基; 或其农业化学可用的盐形式; 条件是当X是C（R）时，R 2不能是任选取代的芳基。
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10.发明申请PYRIDAZINE DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND THEIR USE AS FUNGICIDES 审中-公开吡咯烷酮衍生物，其制备方法及其作为防腐剂的使用公开(公告)号：US20100022526A1
公开(公告)日：2010-01-28
申请号：US12524096
申请日：2008-01-21
IPC分类号： A01N43/58 , C07D237/02 , A01N43/84 , A01P3/00
CPC分类号： C07D237/12 , A01N43/58 , C07D237/14 , C07D237/16 , C07D237/24 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
摘要： The present invention relates to compounds of formula (I) wherein R1, R2, R3 and R4 are as defined in claim 1, which are useful as fungicides.
摘要翻译： 本发明涉及式（I）化合物，其中R 1，R 2，R 3和R 4如权利要求1中所定义，其可用作杀真菌剂。
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