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11. 发明授权

US08455657B2 Process for the preparation of 3-alkylsulfinylbenzoyl derivatives 有权
标题翻译： 3-烷基亚磺酰基苯甲酰基衍生物的制备方法
公开(公告)号：US08455657B2
公开(公告)日：2013-06-04
申请号：US13335662
申请日：2011-12-22
申请人： Mark James Ford , Jan Peter Schmidt , Helmut Kohlhepp
发明人： Mark James Ford , Jan Peter Schmidt , Helmut Kohlhepp
IPC分类号： C07D271/08 , C07D271/10 , C07D271/00 , C07D257/04 , C07D249/00 , C07D231/10 , C07C319/00
CPC分类号： C07C315/04 , C07C2601/16 , C07D231/20 , C07C317/46
摘要： A process is described for the preparation of 3-alkylsulfinylbenzoyl derivatives of the formula (IIIa) by reaction of 3-alkylsulfinylbenzoic acids of the formula (Ib) with compounds of the formula (II) in the presence of a chlorinating agent and a base. In the formulae specified above, Y is a radical such as pyrazolyl and cyclohexanedionyl. R1, R2 and R3 are radicals such as halogen, nitro, cyano and alkyl.
摘要翻译：描述了通过在氯化剂和碱的存在下使式（Ib）的3-烷基亚磺酰基苯甲酸与式（II）的化合物反应来制备式（IIIa）的3-烷基亚磺酰基苯甲酰基衍生物的方法。在上述式中，Y是吡唑基和环己二酰基等基团。 R1，R2和R3是卤素，硝基，氰基和烷基等基团。

12. 发明授权

US07781611B2 Nitro-sulfobenzamides 有权
标题翻译：硝基磺基苯甲酰胺
公开(公告)号：US07781611B2
公开(公告)日：2010-08-24
申请号：US09732006
申请日：2000-12-07
申请人： Mark James Ford , Jan Vermehren
发明人： Mark James Ford , Jan Vermehren
IPC分类号： C07C309/27 , C07C309/29
CPC分类号： C07C303/38 , C07C303/22 , C07C309/59 , C07C311/65 , C07D239/52 , C07D327/04 , C07C311/16 , C07C309/89
摘要： The present invention relates to a compound of the formula (I) wherein R1 is an unsubstituted or substituted hydrocarbon radical having a total of 1 to 10 carbon atoms, preferably 1 to 6 carbon atoms, R2 is an unsubstituted or substituted hydrocarbon radical having a total of 1 to 10 carbon atoms, preferably 1 to 6 carbon atoms, or the group NR1R2 is a heterocyclic ring having 3 to 8 ring atoms which is unsubstituted or substituted and contains the nitrogen atom of the group NR1R2 as ring heteroatom and may also contain one or two further ring heteroatoms from the group consisting of N, O and S, and Q is H or a cation. The compounds of the present invention can advantageously be used for the preparation of sulfonylureas and their precursors such as sulfochlorides or sulfonamides.
摘要翻译：本发明涉及式（I）化合物，其中R 1是总共具有1至10个碳原子，优选1至6个碳原子的未取代或取代的烃基，R 2是未取代或取代的烃基，其具有总计 1〜10个碳原子，优选1〜6个碳原子，或者NR1R2是具有3〜8个环原子的杂环，其未被取代或取代，并且含有NR1R2基团的氮原子作为环杂原子，并且还可以含有一个或另外两个来自N，O和S的环杂原子，Q是H或阳离子。本发明的化合物可以有利地用于制备磺酰脲类及其前体如磺酰氯或磺酰胺。

13. 发明授权

US07026477B1 Process for preparing substituted phenylsulfonylureas from sulfonyl halides 有权
标题翻译：从磺酰卤制备取代苯基磺酰脲的方法
公开(公告)号：US07026477B1
公开(公告)日：2006-04-11
申请号：US10089288
申请日：2000-09-28
申请人： Jan Vermehren , Ernst Schmidt , Mark James Ford , Richard W. G. Foster , Ian A. Bourne
发明人： Jan Vermehren , Ernst Schmidt , Mark James Ford , Richard W. G. Foster , Ian A. Bourne
IPC分类号： C07D251/18
CPC分类号： C07D251/42
摘要： The invention relates to a preparation process for a compound (I) or a salt thereof, in which Q, X*, Y, Z, R, R1, R2 and R3 are as defined in claim 1, which comprises a) ammonolyzing a comp. (II) in which Hal=halogen atom to give (III), pref. (a1) carrying out the reaction in an organic solvent mixture (org. solv. mixture) comprising (1) opt. halogenated aromatic hydrocarbons and (2) polar aprotic solvents, in a weight ratio of solv. (1): solv. (2) of 20:1 to 1:1, (b) phosgenating the comp. (III) with phenylsulfonyl isocyanate of the formula (IV), pref. (b1) in the case X*=halogen, carrying out the reaction with phosgene in an org. solv. in the presence of isocyanates R′-NCO as catalyst, where R′=(subst.) hydrocarbon, with or without addition of an amine base, (c) reacting the resulting compound (IV) in org. solv. with the aminoheterocycle H2N-Het (Het=heterocycle as in (I)) to give the comp. (I) or a salt thereof, pref. (c1) carrying out the reaction in a solv. mixture of opt. halogenated arom. hydrocarbon having a b.p. of more than 110° C. and a polar aprotic solv., where at least one of the preferred partial steps (a1) to (c1) is carried out in the process.
摘要翻译：本发明涉及一种化合物（I）或其盐的制备方法，其中Q，X *，Y，Z，R，R 1，R 2， R 3和R 3如权利要求1所定义，其包括：a）（II），其中Hal =卤素原子以得到（III），优选的。（a1）在包含（1）选择的有机溶剂混合物（有机溶剂混合物）中进行反应。卤代芳烃和（2）极性非质子溶剂，重量比为溶剂。（1）：solv。（2）为20：1至1：1，（b）使化合物光气化。（III）与式（IV）的苯基磺酰基异氰酸酯反应，（b1）在X * =卤素的情况下，在组织中进行与光气的反应。解决方案在异氰酸酯R'-NCO作为催化剂的存在下，其中R'=（取代）烃，具有或不添加胺碱，（c）使所得化合物（IV）在有机溶剂中反应。解决方案与氨基杂环H 2 N-Het（Het =如（I）中的杂环））反应，得到化合物。（I）化合物或其盐。（c1）在溶剂中进行反应。混合选择卤化芳香。 b。超过110℃的极性非质子溶剂，其中优选的部分步骤（a1）至（c1）中的至少一个在该过程中进行。

14. 发明授权

US08969553B2 Method for producing N-sulfonyl-substituted oxindoles 有权
标题翻译： N-磺酰基取代的羟基吲哚的制备方法
公开(公告)号：US08969553B2
公开(公告)日：2015-03-03
申请号：US13995898
申请日：2011-12-19
申请人： Gunter Karig , Mark James Ford , Konrad Siegel , Stefan Schnatterer
发明人： Gunter Karig , Mark James Ford , Konrad Siegel , Stefan Schnatterer
IPC分类号： C07D403/04 , C07D251/20 , A01N43/38 , A01N43/66
CPC分类号： C07D251/20 , A01N43/38 , A01N43/66 , C07D401/04 , C07D403/04
摘要： Process for the selective N-sulfonylation of oxindoles, in particular process for the N-sulfonylation of 3-triazinyloxindoles, and also N-sulfonyl-substituted 3-triazinyloxindoles and the use of N-sulfonyl-substituted oxindoles and of N-sulfonyl-substituted 3-triazinyloxindoles as intermediates for the synthesis of fine chemicals and of active ingredients in the field of pharmacy and agriculture, and also the use of these compounds as active ingredients in the field of agriculture.
摘要翻译：用于N-羟基吲哚的选择性N-磺酰化的方法，特别是3-三嗪基氧基吲哚的N-磺酰化方法，以及N-磺酰基取代的3-三嗪并氧基吲哚和使用N-磺酰基取代的羟基吲哚和N-磺酰基取代的 3-三嗪基氧吲哚作为合成精细化学品和药物和农业领域的活性成分的中间体，以及这些化合物作为农业领域的活性成分的用途。

15. 发明申请

US20140024828A1 Method for producing 2-(triazinylcarbonyl) sulfonanilides 有权
标题翻译： 2-（三嗪基羰基）磺酰苯胺的制备方法
公开(公告)号：US20140024828A1
公开(公告)日：2014-01-23
申请号：US13995886
申请日：2011-12-19
申请人： Gunter Karig , Mark James Ford , Konrad Siegel
发明人： Gunter Karig , Mark James Ford , Konrad Siegel
IPC分类号： C07D251/20
CPC分类号： C07D251/20 , A01N43/38 , A01N43/66 , C07D401/04 , C07D403/04
摘要： The present application relates to a process based on the oxidative ring opening of a compound with oxindole structure for preparation of substituted 2-(triazinylcarbonyl)sulfonanilides of the formula (1-1) proceeding from N-sulfonyl-substituted 3-triazinyloxindole of the formula (2-1), and to the 2-(triazinylcarbonyl)sulfonanilides of the formula (1-1) thus prepared, and to the use thereof as intermediates for the synthesis of fine chemicals and of active ingredients in the agricultural sector.The invention also relates to a multistage process for preparation of N-alkyl-N-[2-(1,3,5-triazin-2-ylcarbonyl)phenyl]alkanesulfonamides of the formula (4-1), proceeding from a 3-(alkylsulfanyl)-1,3-dihydro-2H-indol-2-one of the formula (7-1), wherein the multistage process also comprises, as a component step, the oxidative ring opening mentioned, and to the 2-(triazinylcarbonyl)sulfonanilides of the formula (1-1) which are obtained by the oxidative ring opening and are used as intermediates in the multistage process.
摘要翻译：本申请涉及一种用于制备由式（1-1）取代的2-（三嗪基羰基）磺酰苯胺（具有羟吲哚结构的氧化开环）的方法，所述2-（三嗪基羰基）磺酰苯胺是从下式的N-磺酰基取代的3-三嗪嗪氧基吲哚（2-1），以及由此制备的式（1-1）的2-（三嗪基羰基）磺酰苯胺，以及作为农业领域合成精细化学品和活性成分的中间体的用途。本发明还涉及制备式（4-1）的N-烷基-N- [2-（1,3,5-三嗪-2-基羰基）苯基]烷磺酰胺的多级方法，（7-1）的（烷基硫烷基）-1,3-二氢-2H-吲哚-2-酮，其中多级方法还包括所提及的氧化环开环作为组分步骤，以及2- （1-1）的三嗪基羰基）磺酰苯胺，其通过氧化开环获得并在多级方法中用作中间体。

16. 发明申请

US20110118478A1 PROCESS FOR THE PREPARATION OF OXINDOLES AND ORTHO-SUBSTITUTED ANILINES AND THEIR USE AS INTERMEDIATES FOR SYNTHESES 有权
标题翻译：制备氧化物和取代的苯胺的方法及其作为合成中间体的使用
公开(公告)号：US20110118478A1
公开(公告)日：2011-05-19
申请号：US12769302
申请日：2010-04-28
申请人： Mark James Ford , Gunter Karig
发明人： Mark James Ford , Gunter Karig
IPC分类号： C07D209/34 , C07C323/58 , C07C319/12
CPC分类号： C07D209/34 , C07C323/58
摘要： The present invention relates to processes for the preparation of oxindoles and ortho-substituted anilines and their use as intermediates for syntheses. The invention further relates to a process for the preparation of compounds of formula (4): where a mixture of an aniline (compound of formula Q) is reacted with a thioether (compound of formula W): in the presence of a chlorinating agent and an organic solvent at a reaction temperature in the range above −65° C.In a subsequent process, this compound is further reacted in the presence of an acid catalyst to give the indole of formula (7) or the oxindole of formula (8):
摘要翻译：本发明涉及制备羟吲哚和邻位取代苯胺的方法及其作为合成中间体的用途。本发明还涉及制备式（4）化合物的方法：其中苯胺（式Q化合物）的混合物与硫醚（式W化合物）反应：在氯化剂和在随后的方法中，该化合物在酸催化剂的存在下进一步反应，得到式（7）的吲哚或式（8）的羟吲哚，：

17. 发明申请

US20100305317A1 SYNTHESIS OF BIGUANIDINES AND TRIAZINES, AND BIGUANIDINO-ALUMINIUM COMPLEXES AS INTERMEDIATES 有权
标题翻译：双胍和三嗪的合成及作为中间体的双胍二铝复合物
公开(公告)号：US20100305317A1
公开(公告)日：2010-12-02
申请号：US12808060
申请日：2008-11-25
申请人： Mark James Ford
发明人： Mark James Ford
IPC分类号： C07D251/18 , C07F5/06 , C07D413/04 , C07D401/04
CPC分类号： C07F5/069
摘要： Synthesis of biguanidines and triazines, and biguanidino-aluminium complexes as intermediates Compounds of formula (I) or salts thereof, in which R1, R2, R3, R4, R5, R6, X and Y are defined as in claim 1, can be prepared by a process characterized in that a compound of the formula (II) or a salt thereof, is reacted to a compound of the formula (III) or a salt thereof, and an aluminium (III) source, optionally, in the presence of a protic additive or solvent selected from the group consisting of alcohols or amines. The compounds (I) are suitable to be used for the preparation of heterocyclic compounds corresponding to (I) where the group Al(X)(Y) is replaced with an optionally substituted carbon atom, or s-triazine derivatives thereof.
摘要翻译：双胍和三嗪的合成以及双胍基 - 铝络合物作为中间体可以制备式（I）化合物或其盐，其中R 1，R 2，R 3，R 4，R 5，R 6，X和Y如权利要求1中所定义，通过一种方法，其特征在于式（II）化合物或其盐与式（III）化合物或其盐和铝（III）源反应，任选地，在质子添加剂或选自醇或胺的溶剂。化合物（I）适合用于制备对应于其中基团Al（X）（Y）被任选取代的碳原子取代的（I）或其三嗪衍生物的杂环化合物。

18. 发明授权

US06365739B1 Process for the preparation of 4,6-disubstituted 2-isocyanatopyrimidines and their use as intermediates for active compound syntheses 失效
标题翻译：用于制备4,6-二取代的2-异氰酸基嘧啶的方法及其作为活性化合物合成的中间体的用途
公开(公告)号：US06365739B1
公开(公告)日：2002-04-02
申请号：US09358297
申请日：1999-07-21
申请人： Mark James Ford , Stephen Lachhein
发明人： Mark James Ford , Stephen Lachhein
IPC分类号： C07D23942
CPC分类号： C07D239/545
摘要： Isocyanates of the formula (I) in which X and Y are defined as in formula (I) of claim 1 can be prepared by reacting a compound of the formula (II) or its salts in which X and Y are defined as in formula (I), with 1 to 6 mol of phosgene per mole of compound of the formula (II), in the presence of 2 to 3.5 molar equivalents of a base per mole of compound of the formula (II) and in the presence of an aprotic organic solvent at a reaction temperature in the range from −30 to +60° C. to give the compound of the formula (I). The compounds (I) can be converted by reaction with nucleophiles to give addition products, such as carbamates, ureas and sulfonylureas and corresponding products, e.g. herbicidal sulfonylureas.
摘要翻译：其中X和Y如权利要求1的式（I）中定义的式（I）的异氰酸酯可以通过使式（II）化合物或其盐，其中X和Y如式），在每摩尔式（II）化合物的2至3.5摩尔当量的碱存在下，并且在非质子有机物存在下，每摩尔式（II）的化合物具有1至6摩尔的光气溶剂，反应温度为-30〜+ 60℃，得到式（I）化合物。化合物（I）可以通过与亲核试剂反应而转化，得到加成产物，例如氨基甲酸酯，脲和磺酰脲类及相应的产品，例如。除草磺酰脲类。

19. 发明授权

US6127572A Process for preparing 2-carboxy-5-nitrobenzenesulfonic acid and salts thereof by oxidation 失效
标题翻译：通过氧化制备2-羧基-5-硝基苯磺酸及其盐的方法
公开(公告)号：US6127572A
公开(公告)日：2000-10-03
申请号：US135339
申请日：1998-08-17
申请人： Mark James Ford
发明人： Mark James Ford
IPC分类号： C07B61/00 , C07C303/22 , C07C309/58 , C07C15/16 , C07C315/04
CPC分类号： C07C303/22
摘要： The invention is directed to a simple process for the preparation of the product 2-carboxy-5-nitrobenzenesulfonic acid (=4-nitro-2-sulfo-benzoic acid) or a salt thereof. The product can be prepared by the oxidation reaction of 2-methyl-5-nitrobenzenesulfonic acid with metal hypochlorites in the presence of metal bases from the group consisting of hydroxides and carbonates, essentially with the exclusion of heavy metal salts.
摘要翻译：本发明涉及制备2-羧基-5-硝基苯磺酸（= 4-硝基-2-磺基 - 苯甲酸）或其盐的简单方法。该产物可以通过2-甲基-5-硝基苯磺酸与金属次氯酸盐在金属碱的存在下，由氢氧化物和碳酸盐组成的基团的氧化反应制备，基本上排除了重金属盐。

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