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31. 发明授权

US4740236A N-sulfonyl-imino-thiocarbonic acid diesters as herbicide antagonists for the protection of rice crops 失效
标题翻译： N-磺酰基亚氨基 - 硫代碳酸二酯作为除草剂拮抗剂，用于保护水稻作物
公开(公告)号：US4740236A
公开(公告)日：1988-04-26
申请号：US554734
申请日：1983-11-23
申请人： Werner Topfl
发明人： Werner Topfl
IPC分类号： A01N25/32 , A01N47/42 , C07C335/42 , C07D207/36 , C07D211/54 , C07D213/70 , C07D233/84 , C07D249/12 , C07D263/58 , C07D277/74 , C07D307/30 , C07D307/64 , C07D333/34 , A01N41/10
CPC分类号： C07D213/70 , A01N25/32 , A01N47/42 , C07D207/36 , C07D211/54 , C07D233/84 , C07D249/12 , C07D263/58 , C07D277/74 , C07D307/30 , C07D307/64 , C07D333/34
摘要： N-Sulfonyliminothiocarbonic acid diesters protect rice crops from phytotoxic damage caused by herbicides.
摘要翻译： N-磺酰基亚硫代碳酸二酯保护水稻作物免受除草剂引起的植物毒性损害。

32. 发明授权

US4629802A Sulfonyl carbonoimidates 失效
标题翻译：磺酰基碳酰亚胺酯
公开(公告)号：US4629802A
公开(公告)日：1986-12-16
申请号：US707358
申请日：1985-03-01
申请人： Haukur Kristinsson , Werner Topfl
发明人： Haukur Kristinsson , Werner Topfl
IPC分类号： C07D251/46 , A01N47/36 , A01N47/42 , C07C67/00 , C07C301/00 , C07C303/38 , C07C303/40 , C07C311/63 , C07D239/42 , C07D239/47 , C07D251/16 , C07D521/00 , C07C119/20
CPC分类号： C07D521/00
摘要： A novel process for producing sulfonylureas of the formula I having a herbicidal action and an action regulating plant growth ##STR1## wherein A is an unsubstituted or substituted phenyl, naphthyl, furan, thiophene or pyridine group, E is a nitrogen atom or the methine group, R.sub.a is hydrogen, halogen, C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -haloalkyl, C.sub.1 -C.sub.5 -alkoxy, C.sub.1 -C.sub.5 -haloalkoxy, C.sub.1 -C.sub.5 -alkylthio or C.sub.2 -C.sub.10 -alkoxyalkoxy, and R.sub.b is the same as R.sub.a or is an unsubstituted or substituted amino group, and salts thereof, which process comprises firstly condensing an imidocarbonic acid ester with a sulfonyl chloride of the formula II to the sulfonylimidocarbonic acid diester of the formula IV ##STR2## wherein R is an alkyl group, and reacting this in an ethereal solvent in the presence of sodium hydride or potassium tertbutylate with a 2-aminopyrimidine or 2-amino-1,3,5-triazine of the formula V, and finally reacting the formed sulfonylisourea of the formula VI in an organic solvent with hydrochloric acid to obtain the sulfonylurea of the formula I, and isolating this as such or as a salt; ##STR3## The sulfonylimidocarbonic acid diesters of the formula IV and certain sulfonylisoureas of the formula VI, required as intermediates, are novel compounds. The process has the advantage that no sulfonamides are needed as intermediates.
摘要翻译：一种制备具有除草作用和调节植物生长作用的式I的磺酰脲的新方法，其中A是未取代或取代的苯基，萘基，呋喃，噻吩或吡啶基，E是氮原子或次甲基，R a为氢，卤素，C 1 -C 5 - 烷基，C 1 -C 5 - 卤代烷基，C 1 -C 5 - 烷氧基，C 1 -C 5 - 卤代烷氧基，C 1 -C 5 - 烷硫基或C 2 -C 10 - 烷氧基烷氧基，Rb为与R a相同或为未取代或取代的氨基及其盐，该方法包括首先将亚氨基碳酸酯与式II的磺酰氯缩合成式IV的磺酰亚胺基碳酸二酯其中R是烷基并将其在惰性溶剂中，在氢化钠或叔丁醇钾存在下与式V的2-氨基嘧啶或2-氨基-1,3,5-三嗪反应，最后使形成的式VI的磺酰基异脲在有盐酸的有机溶剂中在式I的磺酰脲中，并将其分离为盐或盐; 作为中间体，式IV的磺酰亚胺基碳酸二酯和式VI的某些磺酰基异脲是新化合物。该方法的优点是不需要磺酰胺作为中间体。

33. 发明授权

US5342823A Sulfonylureas 失效
标题翻译：磺脲类
公开(公告)号：US5342823A
公开(公告)日：1994-08-30
申请号：US18603
申请日：1993-02-17
申请人： Rainer Kuhlmeyer , Werner Topfl , Werner Fory
发明人： Rainer Kuhlmeyer , Werner Topfl , Werner Fory
IPC分类号： A01N47/36 , C07D213/80 , C07D231/18 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D521/00 , F16N11/04 , F16N11/08 , C07D407/14 , A01N43/54
CPC分类号： C07D521/00 , A01N47/36 , C07D405/12 , C07D409/12 , F16N11/04 , F16N11/08 , F16N2230/10
摘要： N-Arylsulfonyl-N'-pyrimidinyl-and N'-triazinylureas of formula I ##STR1## wherein Q is ##STR2## R is hydrogen or methyl; R.sub.1 is hydrogen, fluoro, chloro, C.sub.1 -C.sub.4 alkyl or methoxy;R.sub.2 is hydrogen, fluoro or chloro;R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are each independently of one another hydrogen or C.sub.1-C.sub.4 alkyl;R.sub.8, R.sub.9, R.sub.10, R.sub.11 and R.sub.12 are each independently of one another hydrogen or C.sub.1 -C.sub.4 alkyl;R.sub.13, R.sub.14, R.sub.15, R.sub.16 and R.sub.17 are each independently of one another hydrogen or C.sub.1 -C.sub.4 alkyl;Z is methyl or 2-pyridyl;E is methine or nitrogen;X is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.1 -C.sub.4 haloalkylthio, C.sub.1 -C.sub.4 alkylthio,C.sub.2 -C.sub.5 alkoxyalkyl, C.sub.2 -C.sub.5 alkoxyalkoxy, C.sub.2 -C.sub.5 alkylthioalkyl or cyclopropyl;Y is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 haloalkylthio,C.sub.1 -C.sub.4 alkylthio, halogen, C.sub.2 -C.sub.5 alkoxyalkyl, C.sub.2 -C.sub.5 alkoxyalkoxy, amino, C.sub.1 -C.sub.3 alkylamino or di-(C.sub.1 -C.sub.3 alkyl)amino;and the salts of these compounds with amines, alkali metal or alkaline earth metal bases or with quaternary ammonium bases, have good pre-and postemergence selective herbicidal and growth regulating properties.
摘要翻译：（Q）（Q 3）（Q 3）（Q 3）R 3是氢或甲基; R 3是氢或甲基; R 3是氢或甲基。 R 1是氢，氟，氯，C 1 -C 4烷基或甲氧基; R2是氢，氟或氯; R3，R4，R5，R6和R7各自独立地为氢或C1-C4烷基; R8，R9，R10，R11和R12各自独立地为氢或C1-C4烷基; R 13，R 14，R 15，R 16和R 17各自独立地为氢或C 1 -C 4烷基; Z是甲基或2-吡啶基; E是次甲基或氮; X是C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷氧基，C 1 -C 4卤代烷硫基，C 1 -C 4烷硫基，C 2 -C 5烷氧基烷基，C 2 -C 5烷氧基烷氧基，C 2 -C 5烷硫基烷基或环丙基; Y是C1-C4烷基，C1-C4烷氧基，C1-C4卤代烷氧基，C1-C4卤代烷基，C1-C4卤代烷硫基，C1-C4烷硫基，卤素，C2-C5烷氧基烷基，C2-C5烷氧基烷氧基，氨基，C1-C3烷基氨基或二 - （C1-C3烷基）氨基 ; 并且这些化合物与胺，碱金属或碱土金属碱或季铵碱的盐具有良好的芽前和芽后选择性除草和生长调节性质。

34. 发明授权

US4902336A Herbicidal compositions 失效
标题翻译：除草成分
公开(公告)号：US4902336A
公开(公告)日：1990-02-20
申请号：US245601
申请日：1988-09-19
申请人： Werner Topfl
发明人： Werner Topfl
IPC分类号： C07D249/16 , A01N47/34 , A01N47/36 , A01N57/08 , C07D239/42 , C07D239/46 , C07D239/47 , C07D251/16 , C07D251/18 , C07D401/12 , C07D403/12 , C07D417/12 , C07D521/00 , C07F9/6512 , C07F9/6521 , C07F9/6558
CPC分类号： C07D239/42 , A01N47/36 , A01N57/08 , C07D239/47 , C07D401/12 , C07D403/12 , C07D417/12 , C07D521/00 , C07F9/65212
摘要： N-Arylsulfonyl-N'-(4-mercaptomethyl-pyrimidinyl-ureas of the formula ##STR1## (symbols in this formula defined herein) and the salts of these compounds with amines, alkali metal bases or alkaline-earth metal bases or with ammonium bases, have good pre- and post-emergence-selective, herbicidal and growth-regulating properties.

35. 发明授权

US4017638A Iso-(thio)-urea derivatives 失效
标题翻译：异硫代脲衍生物
公开(公告)号：US4017638A
公开(公告)日：1977-04-12
申请号：US663413
申请日：1976-03-03
申请人： Volker Dittrich , Werner Topfl , Odd Kristiansen
发明人： Volker Dittrich , Werner Topfl , Odd Kristiansen
IPC分类号： A01N47/42 , C07C67/00 , C07C301/00 , C07C303/36 , C07C311/54 , C07C311/63 , C07C335/42 , C07C123/00
CPC分类号： A01N47/42 , C07C311/63 , C07C335/42
摘要： Iso-(thio)-urea derivatives of the formula ##STR1## wherein R.sub.1 and R.sub.2 each represent C.sub.1 -C.sub.5 -alkyl or phenyl or benzyl mono-, di- or trisubstituted by halogen, trifluoromethyl, nitro and/or methyl, andX represents oxygen or sulphur, processes for their production and their use in pest control.
摘要翻译：其中R 1和R 2各自表示C 1 -C 5烷基或被卤素，三氟甲基，硝基和/或甲基单，二或三取代的苯基或苄基，X代表氧气或硫磺，其生产过程及其在病虫害防治中的应用。

36. 发明授权

US5215570A Sulfamoylphenylureas 失效
标题翻译：磺酰基苯基脲
公开(公告)号：US5215570A
公开(公告)日：1993-06-01
申请号：US637097
申请日：1991-01-03
申请人： Urs Burckhardt , Raafat Soliman , Werner Topfl , Hans-Rudolf Waespe
发明人： Urs Burckhardt , Raafat Soliman , Werner Topfl , Hans-Rudolf Waespe
IPC分类号： A01N25/32 , C07C311/51 , C07D213/81 , C07D307/68 , C07D333/38
CPC分类号： C07D213/81 , A01N25/32 , C07C311/51 , C07D307/68 , C07D333/38
摘要： The N-acylsulfamoylphenylureas of formula I below are suitable as counter-agents (antidotes or safeners) for protecting cultivated plants from the phytotoxic action of herbicides. Suitable crops are preferably cereals, soybeans, sorghum, maize and rice, and suitable herbicides are sulfonylureas, chloroacetanilides and aryloxyphenoxypropionic acid derivatives.The N-acylsulfamoylphenylureas have the formula I ##STR1## wherein A is a radical selected from the group ##STR2## R.sub.1 is C.sub.1 -C.sub.4 -alkoxy or each of R.sub.1 and R.sub.2, independently of the other, is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, ##STR3## or C.sub.1 -C.sub.4 alkyl substituted by C.sub.1 -C.sub.4 alkoxy or by ##STR4## or R.sub.1 and R.sub.2 together form a C.sub.4 -C.sub.6 alkylene bridge, or a C.sub.4 -C.sub.6 alkylene bridge interrupted by oxygen, sulfur, SO, SO.sub.2, NH or by --N(C.sub.1 -C.sub.4 alkyl)-, R.sub.3 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.a to R.sub.h, R.sub.x and R.sub.y are as defined in the disclosure.
摘要翻译：下式I的N-酰基氨磺酰基苯基脲适用于保护栽培植物免受除草剂植物毒性作用的反作用剂（解毒剂或安全剂）。合适的作物优选是谷物，大豆，高粱，玉米和水稻，合适的除草剂是磺酰脲类，氯乙酰苯胺和芳氧基苯氧基丙酸衍生物。 N-酰基磺酰基苯基脲具有式I（I）其中A是选自下列基团的基团：R1是C1-C4-烷氧基或R1和R2中的每一个，独立于另一个，是氢，C1-C8烷基，C3-C8环烷基，C3-C6链烯基，C3-C6炔基，或C1-C4烷氧基取代的C1-C4烷基，或者由R1和R2一起形成C4-C6亚烷基桥，或由氧，硫，SO，SO2，NH或-N（C1-C4烷基） - 间隔的C4-C6亚烷基桥，R3是氢或C1-C4烷基，Ra到Rh，Rx和Ry如本公开所定义。

37. 发明授权

US4992434A Microbicidal composition 失效
标题翻译：杀菌组合物
公开(公告)号：US4992434A
公开(公告)日：1991-02-12
申请号：US336166
申请日：1989-04-11
申请人： Werner Topfl , Robert Nyfeler , Werner Fory
发明人： Werner Topfl , Robert Nyfeler , Werner Fory
IPC分类号： A01N43/78 , C07D277/56 , C07D277/60 , C07D417/06 , C07D417/12 , C07D493/04 , C07F9/6539
CPC分类号： C07D277/60 , A01N43/78 , C07D277/56 , C07D417/06 , C07D417/12 , C07D493/04 , C07F9/6539
摘要： A microbicidal compostion contains as active ingredient 2-chloro-4-trifluoromethylthiazol-5-carbonic acid derivatives of the formula I ##STR1## R is organic radical with up to 40 carbon atoms, which optionally contains nitrogen, oxygen or sulfur atoms and which can be transformed by hydrolosis or oxydation into the directly to the thiazol ring bound carboxyl rest. These compounds have good microbicidal activity and are used for the control and prevention of infestation of plants by phytophathogenic microorganisms.
摘要翻译：杀微生物组合物含有作为活性成分的式I的2-氯-4-三氟甲基噻唑-5-碳酸衍生物（I）R是具有多达40个碳原子的有机基团，其任选地含有氮，氧或硫原子并且其可以通过水痘病毒或氧化反应直接转化成噻唑环结合的羧基。这些化合物具有良好的杀菌活性，用于通过植物致病微生物控制和预防植物侵染。

38. 发明授权

US4921955A Process for the synthesis of 1-substituted imidazole-5-carboxylic acids and carboxylic acid derivatives 失效
标题翻译：合成1-取代咪唑-5-羧酸和羧酸衍生物的方法
公开(公告)号：US4921955A
公开(公告)日：1990-05-01
申请号：US136167
申请日：1987-12-18
申请人： Werner Topfl
发明人： Werner Topfl
IPC分类号： A01N43/50 , C07C67/00 , C07C239/00 , C07C261/04 , C07D215/38 , C07D215/40 , C07D217/02 , C07D233/90 , C07D307/79 , C07D311/68 , C07D311/96 , C07D333/58 , C07D409/04
CPC分类号： C07D409/04 , C07C261/04 , C07D233/90 , C07C2102/08 , C07C2102/10
摘要： The invention relates to a process for the preparation of 1,5-disubstituted imidazoles of the formula ##STR1## by alkylation of an N-cyanoformamidine of the formula IIX--NH--CH.dbd.N--CH (II)to form an N,N-disubstituted N'-cyanoformamidine of the formula ##STR2## which is cyclised under the action of bases to form a 4-aminoimidazole of the formula ##STR3## and then reduced to form the product of the formula I. The invention relates also to a special process for the reduction of the aminoimidazole V to I, and to intermediate compounds for carrying out this process and to processes for the preparation of the intermediate compounds.The meaning of the substituents X and L is explained in detail in the text.
摘要翻译：本发明涉及通过将式II的X-NH-CH = N-CH（II）的N-氰基甲脒烷基化制备式（I）的1,5-二取代咪唑的方法，以形成式（Ⅳ）的N，N-二取代的N'-氰基甲脒，其在碱的作用下环化以形成式（Ⅴ）的4-氨基咪唑，然后还原形成本发明还涉及将氨基咪唑V还原成I的特殊方法以及用于进行该方法的中间体化合物和中间体化合物的制备方法。取代基X和L的含义在文中详细解释。

39. 发明授权

US4786315A Herbicidal compositions 失效
标题翻译：除草成分
公开(公告)号：US4786315A
公开(公告)日：1988-11-22
申请号：US919514
申请日：1986-11-24
申请人： Werner Topfl
发明人： Werner Topfl
IPC分类号： C07D249/16 , A01N47/34 , A01N47/36 , A01N57/08 , C07D239/42 , C07D239/46 , C07D239/47 , C07D251/16 , C07D251/18 , C07D401/12 , C07D403/12 , C07D417/12 , C07D521/00 , C07F9/6512 , C07F9/6521 , C07F9/6558 , C07D251/22 , A01N43/66
CPC分类号： C07D239/42 , A01N47/36 , A01N57/08 , C07D239/47 , C07D401/12 , C07D403/12 , C07D417/12 , C07D521/00 , C07F9/65212
摘要： N-Arylsulfonyl-N'-(4-mercaptomethyl-pyrimidinyl- and -triazinyl)-ureas of the formula: ##STR1## and the salts of these compounds with amines, alkali metal bases or alkaline-earth metal bases or with ammonium bases, have good pre- and post-emergence-selective, herbicidal and growth-regulating properties.
摘要翻译：具有下式的N-芳基磺酰基-N' - （4-巯基甲基 - 嘧啶基 - 和三嗪基） - 脲和这些化合物与胺，碱金属碱或碱土金属碱或铵碱的盐，具有良好的芽前和芽后选择性，除草和生长调节性质。

40. 发明授权

US4521597A Process for producing sulfonylureas having a herbicidal action 失效
标题翻译：制备具有除草作用的磺酰脲的方法
公开(公告)号：US4521597A
公开(公告)日：1985-06-04
申请号：US542312
申请日：1983-10-14
申请人： Haukur Kristinsson , Werner Topfl
发明人： Haukur Kristinsson , Werner Topfl
IPC分类号： C07D251/46 , A01N47/36 , A01N47/42 , C07C67/00 , C07C301/00 , C07C303/38 , C07C303/40 , C07C311/63 , C07D239/42 , C07D239/47 , C07D251/16 , C07D521/00 , C07D251/18 , C07D239/69 , C07D251/52
CPC分类号： C07D521/00
摘要： A novel process for producing sulfonylureas of the formula I having a herbicidal action and an action regulating plant growth ##STR1## wherein A is an unsubstituted or substituted phenyl, naphthyl, furan, thiophene or pyridine group, E is a nitrogen atom or the methine group, R.sub.a is hydrogen, halogen, C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -haloalkyl, C.sub.1 -C.sub.5 -alkoxy, C.sub.1 -C.sub.5 -haloalkoxy, C.sub.1 -C.sub.5 -alkylthio or C.sub.2 -C.sub.10 -alkoxyalkoxy, and R.sub.b is the same as R.sub.a or is an unsubstituted or substituted amino group, and salts thereof, which process comprises firstly condensing an imidocarbonic acid ester with a sulfonyl chloride of the formula II to the sulfonylimidocarbonic acid diester of the formula IV ##STR2## wherein R is an alkyl group, and reacting this in an ethereal solvent in the presence of sodium hydride or potassium tertbutylate with a 2-aminopyrimidine or 2-amino-1,3,5-triazine of the formula V, and finally reacting the formed sulfonylisourea of the formula VI in an organic solvent with hydrochloric acid to obtain the sulfonylurea of the formula I, and isolating this as such or as a salt; ##STR3## The sulfonylimidocarbonic acid diesters of the formula IV and certain sulfonylisoureas of the formula VI, required as intermediates, are novel compounds. The process has the advantage that no sulfonamides are needed as intermediates.
摘要翻译：一种制备具有除草作用和调节植物生长作用的式I的磺酰脲的新方法，其中A是未取代或取代的苯基，萘基，呋喃，噻吩或吡啶基，E是氮原子或次甲基，R a为氢，卤素，C 1 -C 5 - 烷基，C 1 -C 5 - 卤代烷基，C 1 -C 5 - 烷氧基，C 1 -C 5 - 卤代烷氧基，C 1 -C 5 - 烷硫基或C 2 -C 10 - 烷氧基烷氧基，Rb为与R a相同或为未取代或取代的氨基及其盐，该方法包括首先将亚氨基碳酸酯与式II的磺酰氯缩合成式IV的磺酰亚胺基碳酸二酯其中R是烷基并将其在惰性溶剂中，在氢化钠或叔丁醇钾存在下与式V的2-氨基嘧啶或2-氨基-1,3,5-三嗪反应，最后使形成的式VI的磺酰基异脲在有盐酸的有机溶剂中在式I的磺酰脲中，并将其分离为盐或盐; 作为中间体，式IV的磺酰亚胺基碳酸二酯和式VI的某些磺酰基异脲是新化合物。该方法的优点是不需要磺酰胺作为中间体。

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