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11. 发明申请

US20080076920A1 PREPARATION OF THIAZOLES 失效
标题翻译：制备THIAZOLES
公开(公告)号：US20080076920A1
公开(公告)日：2008-03-27
申请号：US11947891
申请日：2007-11-30
申请人： Thomas Pitterna , Henry Szczepanski , Peter Maienfisch , Ottmar Huter , Thomas Rapold , Marcel Senn , Thomas Gobel , Anthony O'Sullivan
发明人： Thomas Pitterna , Henry Szczepanski , Peter Maienfisch , Ottmar Huter , Thomas Rapold , Marcel Senn , Thomas Gobel , Anthony O'Sullivan
IPC分类号： C07D417/02 , C07D277/36 , C07D417/14
CPC分类号： C07D277/32 , C07D277/16 , C07D277/36 , C07D277/70 , C07D277/74
摘要： The present disclosure is directed to a process for the preparation of a compound having the formula: wherein R is unsubstituted or substituted C1-C12alkyl, unsubstituted or substituted C2-C4alkenyl, unsubstituted or substituted C2-C4alkynyl, unsubstituted or substituted C3-C6cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted heteroaryl, or —SR1; R1 is unsubstituted or substituted C1-C12alkyl, unsubstituted or substituted C2-C4alkenyl, unsubstituted or substituted C2-C4alkynyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl or unsubstituted or substituted heteroaryl; and X is a selected leaving group that is not halogen, and may specifically be methylsulfonate, trifluoromethylsulfonate, and p-toluenesulfonate. These compounds are valuable intermediates useful in the synthesis of compounds having pesticidal activity. Generally, the process includes reacting a water-removing reagent, with a compound having the formula Water-removing agents that may be used include thionyl chloride (SOCl2), thionyl bromide (SOBr2), phosphorus oxychloride (POCl3), phosphorus oxybromide (POBr3), phosphorus pentachloride or a sulfonic acid chloride or bromide.
摘要翻译：本公开涉及制备具有下式的化合物的方法：其中R是未取代或取代的C 1 -C 12烷基，未取代或取代的C 1 -C 12烷基，未取代或取代的C 2 -C 4炔基，未取代或取代的C 1 -C 4烷基， 3个C 6环烷基，未取代或取代的芳基，未取代或取代的杂芳基或-SR 1 N; R 1是未取代或取代的C 1 -C 12烷基，未取代或取代的C 2 -C 3 未取代或取代的C 2 -C 4炔基，未取代或取代的环烷基，未取代或取代的芳基或未取代或取代的杂芳基; X是不是卤素的选择的离去基团，可以具体为甲基磺酸酯，三氟甲基磺酸酯和对甲苯磺酸酯。这些化合物是有用的合成具有杀虫活性的化合物的中间体。通常，该方法包括使除水试剂与具有式的化合物反应可以使用的除水剂包括亚硫酰氯（SOCl 2/2），亚硫酰溴（SO 2 R 2）（POCl 3 3），三溴氧化磷（POBr 3 N），五氯化磷或磺酰氯或溴化物。

12. 发明申请

US20070055063A1 PREPARATION OF THIAZOLES 失效
标题翻译：制备THIAZOLES
公开(公告)号：US20070055063A1
公开(公告)日：2007-03-08
申请号：US11552255
申请日：2006-10-24
申请人： Thomas Pitterna , Henry Szczepanski , Peter Maienfisch , Ottmar Huter , Thomas Rapold , Marcel Senn , Thomas Gobel , Anthony O'Sullivan
发明人： Thomas Pitterna , Henry Szczepanski , Peter Maienfisch , Ottmar Huter , Thomas Rapold , Marcel Senn , Thomas Gobel , Anthony O'Sullivan
IPC分类号： C07D417/02
CPC分类号： C07D277/32 , C07D277/16 , C07D277/36 , C07D277/70 , C07D277/74
摘要： A process for the preparation of a compound of the formula and, where applicable, its E/Z-isomers, mixtures of E/Z-isomers and/or tautomers and acid addition products thereof, in each case in free form or in salt form, wherein: R is unsubstituted or substituted C1-C12alkyl, unsubstituted or substituted C2-C4alkenyl, unsubstituted or substituted C2-C4alkynyl, unsubstituted or substituted C3-C6cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted heteroaryl, or —SR1; R1 is unsubstituted or substituted C1-C12alkyl, unsubstituted or substituted C2-C4alkenyl, unsubstituted or substituted C2-C4alkynyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl or unsubstituted or substituted heteroaryl; and X is a leaving group; The process comprises reacting a compound of the formula: with a halogenating agent or a sulfonylating agent. Alternatively, when X is a selected halogen, the process can comprise reacting a compound of the formula with a compound having a formula selected from the group consisting of halogen-C(═O)—O—C1-C8alkyl; halogen-C(═O)—O-aryl; and halogen-C(═O)—O-benzyl.
摘要翻译：制备下式化合物及其E / Z-异构体的方法，E / Z-异构体和/或互变异构体的混合物及其酸加成产物，各自为游离形式或盐形式，其中：R是未取代或取代的C 1 -C 12烷基，未取代或取代的C 2 -C 4 烯基，未取代或取代的C 2 -C 4炔基，未取代或取代的C 3 -C 6环烷基，未取代或取代的芳基，未取代或取代的杂芳基或-SR 1 N; R 1是未取代或取代的C 1 -C 12烷基，未取代或取代的C 2 -C 3 未取代或取代的C 2 -C 4炔基，未取代或取代的环烷基，未取代或取代的芳基或未取代或取代的杂芳基; X为离去群; 该方法包括使下式化合物与卤化剂或磺酰化剂反应。或者，当X是选择的卤素时，该方法可以包括使下式的化合物与具有选自以下的式的化合物反应：卤素-C（ - ） - O-C 1 -C 烷基; 卤素-C（ - ） - O-芳基; 和卤素-C（ - ） - O-苄基。

13. 发明授权

US06265585B1 Process for the preparation of thiazole derivatives 失效
标题翻译：噻唑衍生物的制备方法
公开(公告)号：US06265585B1
公开(公告)日：2001-07-24
申请号：US09341716
申请日：1999-07-15
申请人： Thomas Pitterna , Peter Maienfisch , David John Wadsworth , Laurenz Gsell , Thomas Rapold , Henry Szczepanski
发明人： Thomas Pitterna , Peter Maienfisch , David John Wadsworth , Laurenz Gsell , Thomas Rapold , Henry Szczepanski
IPC分类号： C07D27732
CPC分类号： C07D277/32
摘要： A process for the preparation of a compound of formula (I), wherein X is a leaving group; which process comprises, a) for the preparation of a compound of formula (I) wherein X is —OS(═O)2A and A is as defined in the specification, reacting a compound of formula (II) with a sulfonylating agent; or, b) for the preparation of a compound of formula (I) wherein X is iodine, reacting a compound of formula (III) with an iodinating agent, preferably sodium iodide; or, c) for the preparation of a compound of formula (I) whrein X is bromine, reacting a compound of formula (IV) with a brominating agent; or, d) for the preparation of a compound (I) wherein X is chlorine or bromine, reacting a compound (V), wherein R and X are as defined in the specification, with a chlorinating agent, a compound of formula (Ib), the use thereof and a process for the preparation of a compound of formula (II) and a compound of formula (A) are described.
摘要翻译：一种制备式（I）化合物的方法，其中X是离去基团; 该方法包括a）制备式（I）化合物，其中X为-OS（= O）2A且A如说明书中所定义，式（II）化合物与磺酰化剂反应; 或b）制备其中X为碘的式（I）化合物，使式（III）化合物与碘化剂，优选碘化钠反应; 或者，c）制备式（I）化合物，其中X是溴，式（Ⅳ）化合物与溴化剂反应; 或者d）制备其中X为氯或溴的化合物（I），其中R和X如说明书中所定义的化合物（Ⅴ）与氯化剂，式（Ib）化合物反应，描述了其用途和制备式（II）化合物和式（A）化合物的方法。

14. 发明授权

US06518433B1 Process for the preparation of nitroguanidine derivatives 失效
标题翻译：制备硝基胍衍生物的方法
公开(公告)号：US06518433B1
公开(公告)日：2003-02-11
申请号：US09646441
申请日：2000-09-18
申请人： Peter Maienfisch , Thomas Rapold , Henry Szczepanski
发明人： Peter Maienfisch , Thomas Rapold , Henry Szczepanski
IPC分类号： C07D40112
CPC分类号： C07D277/32 , C07D213/61
摘要： A process for the production of a compound of formula (I) wherein R1 is hydrogen or C1-C4-alkyl; R2 is hydrogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkinyl, C3-C6-cycloalkyl or a radical —CH2B; A is selected from the group consisiting of 2-chloropyrid-5-yl, tetrahydrofuran-3 -yl, 5-methyl-tetrahydrofuran-3-yl or 2-chlorothiazol-5-yl; and B is phenyl, 3-pyridyl or thiazolyl, which are optionally substituted by one to three substituents selected from the group consisting of C1-C3-alkyl, C1-C3-halogenalkyl, cyclopropyl, halogencyclopropyl, C2-C3-alkenyl, C2-C3-alkinyl, C1-C3-alkoxy, C2-C3-halogenalkenyl, C2-C3-halogenalkinyl, C1-C3-halogenalkoxy, C1-C3-alkylthio, C1-C3-halogenalkylthio, allyloxy, propargyloxy, allylthio, propargylthio, halogenallyloxy, halogenallylthio, halogen, cyano or nitro; and optionally the possible E/Z isomers, E/Z isomeric mixtures and/or tautomers thereof, respectively in free form or in salt form; characterised in that a compound of formula (II) wherein R1, R2 and A have the same significances as in formula (I), and X is O or S; is hydrolysed with a strong acid at a pH below 2; at a temperature between 50 and 100° C; and in a solvent selected from the group consisting of water, alcohols, ethers or mixtures thereof. The compounds of formula (I) are suitable for the preparation of pesticides.
摘要翻译：制备其中R 1为氢或C 1 -C 4 - 烷基的式（I）化合物的方法; R 2为氢，C 1 -C 6 - 烷基，C 2 -C 6 - 烯基，C 2 -C 6 - 炔基，C 3 -C 6 - 环烷基或基团-CH 2 B; A选自2-氯吡啶-5-基，四氢呋喃-3-基，5-甲基 - 四氢呋喃-3-基或2-氯噻唑-5-基; 并且B是苯基，3-吡啶基或噻唑基，其任选被一至三个选自C 1 -C 3 - 烷基，C 1 -C 3 - 卤代烷基，环丙基，卤素基，C 2 -C 3 - 烯基，C 2 -C 3 - 烷基，C 1 -C 3 - 烷氧基，C 2 -C 3 - 卤代链烯基，C 2 -C 3 - 卤代炔基，C 1 -C 3 - 卤代烷氧基，C 1 -C 3 - 烷硫基，C 1 -C 3 - 卤代烷硫基，烯丙氧基，炔丙氧基，烯丙硫基，炔丙硫基，卤代烯氧基，卤代烯硫基，卤素，氰基或硝基;以及任选分别为游离形式或盐形式的可能的E / Z异构体，E / Z异构体混合物和/或互变异构体;其特征在于式（II）化合物，其中R 1，R 2和 A具有与式（I）中相同的含义，X为O或S;在pH低于2的情况下用强酸水解; 温度在50至100℃之间; 和在选自水，醇，醚或其混合物的溶剂中。式（I）化合物适用于制备农药。

15. 发明授权

US5763481A Vinylcarboxylic acid derivatives 失效
标题翻译：乙烯基羧酸衍生物
公开(公告)号：US5763481A
公开(公告)日：1998-06-09
申请号：US678002
申请日：1996-07-10
申请人： Peter Maienfisch , Manfred Boger , Thomas Pitterna , Henry Szczepanski
发明人： Peter Maienfisch , Manfred Boger , Thomas Pitterna , Henry Szczepanski
IPC分类号： A01C1/00 , A01N37/18 , A01N37/22 , A01N37/24 , A01N41/06 , A01N41/10 , A01N55/00 , A01N55/10 , C07C51/38 , C07C57/52 , C07C57/76 , C07C69/63 , C07C69/65 , C07C233/09 , C07C233/12 , C07C233/33 , C07C233/55 , C07C237/42 , C07C255/60 , C07C311/46 , C07C317/38 , C07C317/40 , C07C323/37 , C07C323/41 , C07D213/70 , C07D239/38 , C07D291/00 , C07D295/16 , C07D295/192 , C07F7/08 , C07F7/12 , C07F7/18
CPC分类号： C07D295/192 , A01N37/22 , A01N37/24 , A01N41/06 , A01N41/10 , A01N55/00 , C07C233/09 , C07C233/33 , C07C233/55 , C07C237/42 , C07C255/60 , C07C311/46 , C07C317/40 , C07C323/41 , C07C51/38 , C07C57/52 , C07C69/63 , C07C69/65 , C07F7/0818 , C07F7/184 , C07C2101/02 , C07C2101/14 , C07C2101/18
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is C.sub.3 -C.sub.8 cycloalkyl, halo-C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.6 alkyl, halo-C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.6 alkyl, --Si(R.sub.3).sub.3, --S--R.sub.4, --SO.sub.2 --R.sub.6 or --CO--R.sub.9 ;R.sub.2 is halogen, C.sub.1 -C.sub.4 alkyl or CF.sub.3, the substituents R.sub.2 being identical or different when n is 2; R.sub.3 each independently of the others is C.sub.1 -C.sub.6 alkyl, halo-C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or phenyl; R.sub.4 is aryl or heteroaryl each of which is unsubstituted or substituted; R.sub.6 is unsubstituted or substituted C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.1 -C.sub.20 -alkoxy, C.sub.2 -C.sub.6 alkenyloxy, C.sub.2 -C.sub.6 alkynyloxy, C.sub.1 -C.sub.4 alkylthio, aryl, aryloxy or arylthio, or is optionally substituted amino; R.sub.9 is hydroxy, unsubstituted or substituted C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.8 cycloalkyl, aryl or aryloxy, or is optionally substituted amino; R.sub.12 is hydrogen or unsubstituted or substituted C.sub.1 -C.sub.10 alkyl; m is 1,3,5,7,9 or 11; n is 0,1 or 2; X is fluorine or chlorine; and Y is hydrogen, fluorine or methyl; ps in free form or in salt form, can be used as pesticides and can be prepared in a manner known per se.
摘要翻译：式（I）的化合物，其中R 1是C 3 -C 8环烷基，卤代-C 3 -C 8环烷基，C 3 -C 8环烷基-C 1 -C 6烷基，卤代-C 3 -C 8环烷基-C 1 -C 6烷基，-Si（R 3）3，-S -R4，-SO2-R6或-CO-R9; R2是卤素，C1-C4烷基或CF3，当n为2时，取代基R2相同或不同; R 3各自独立地为C 1 -C 6烷基，卤代-C 1 -C 6烷基，C 1 -C 6烷氧基或苯基; R4是芳基或杂芳基，其各自为未取代或取代的; R 6是未取代的或取代的C 1 -C 10烷基，C 2 -C 6烯基，C 2 -C 6炔基，C 1 -C 20烷氧基，C 2 -C 6烯氧基，C 2 -C 6炔氧基，C 1 -C 4烷硫基，芳基，芳氧基或芳硫基，或任选取代的氨基; R 9为羟基，未取代或取代的C 1 -C 10烷基，C 2 -C 6烯基，C 2 -C 6炔基，C 3 -C 8环烷基，芳基或芳氧基，或任选取代的氨基; R 12是氢或未取代的或取代的C 1 -C 10烷基; m为1,3,5,7,9或11; n为0,1或2; X是氟或氯; Y为氢，氟或甲基; ps为游离形式或盐形式，可用作农药，可以以本身已知的方式制备。

16. 发明授权

US5545630A Vinylcarboxylic acid derivatives 失效
标题翻译：乙烯基羧酸衍生物
公开(公告)号：US5545630A
公开(公告)日：1996-08-13
申请号：US462450
申请日：1995-06-05
申请人： Peter Maienfisch , Manfred B oger , Thomas Pitterna , Henry Szczepanski
发明人： Peter Maienfisch , Manfred B oger , Thomas Pitterna , Henry Szczepanski
IPC分类号： A01C1/00 , A01N37/18 , A01N37/22 , A01N37/24 , A01N41/06 , A01N41/10 , A01N55/00 , A01N55/10 , C07C51/38 , C07C57/52 , C07C57/76 , C07C69/63 , C07C69/65 , C07C233/09 , C07C233/12 , C07C233/33 , C07C233/55 , C07C237/42 , C07C255/60 , C07C311/46 , C07C317/38 , C07C317/40 , C07C323/37 , C07C323/41 , C07D213/70 , C07D239/38 , C07D291/00 , C07D295/16 , C07D295/192 , C07F7/08 , C07F7/12 , C07F7/18 , C07F7/10
CPC分类号： C07D295/192 , A01N37/22 , A01N37/24 , A01N41/06 , A01N41/10 , A01N55/00 , C07C233/09 , C07C233/33 , C07C233/55 , C07C237/42 , C07C255/60 , C07C311/46 , C07C317/40 , C07C323/41 , C07C51/38 , C07C57/52 , C07C69/63 , C07C69/65 , C07F7/0818 , C07F7/184 , C07C2101/02 , C07C2101/14 , C07C2101/18
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is C.sub.3 -C.sub.8 cycloalkyl, halo-C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.6 alkyl, halo-C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.6 alkyl, --Si(R.sub.3).sub.3, --S--R.sub.4, --SO.sub.2 --R.sub.6 or --CO--R.sub.9 ;R.sub.2 is halogen, C.sub.1 -C.sub.4 alkyl or CF.sub.3, the substituents R.sub.2 being identical or different when n is 2;R.sub.3 each independently of the others is C.sub.1 -C.sub.6 alkyl, halo-C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or phenyl;R.sub.4 is aryl or heteroaryl each of which is unsubstituted or substituted;R.sub.6 is unsubstituted or substituted C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.1 -C.sub.20 alkoxy, C.sub.2 -C.sub.6 alkenyloxy, C.sub.2 -C.sub.6 alkynyloxy, C.sub.1 -C.sub.4 alkylthio, aryl, aryloxy or arylthio, or is optionally substituted amino;R.sub.9 is hydroxy, unsubstituted or substituted C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.8 cycloalkyl, aryl or aryloxy, or is optionally substituted amino;R.sub.12 is hydrogen or unsubstituted or substituted C.sub.1 -C.sub.10 alkyl;m is 1, 3, 5, 7, 9 or 11;n is 0, 1 or 2;X is fluorine or chlorine; andY is hydrogen, fluorine or methyl;in free form or in salt form, can be used as pesticides and can be prepared in a manner known per se.
摘要翻译：式（I）的化合物，其中R 1是C 3 -C 8环烷基，卤代-C 3 -C 8环烷基，C 3 -C 8环烷基-C 1 -C 6烷基，卤代-C 3 -C 8环烷基-C 1 -C 6烷基，-Si（R 3）3，-S -R4，-SO2-R6或-CO-R9; R2是卤素，C1-C4烷基或CF3，当n为2时，取代基R2相同或不同; R 3各自独立地为C 1 -C 6烷基，卤代-C 1 -C 6烷基，C 1 -C 6烷氧基或苯基; R4是芳基或杂芳基，其各自为未取代或取代的; R 6是未取代的或取代的C 1 -C 10烷基，C 2 -C 6烯基，C 2 -C 6炔基，C 1 -C 20烷氧基，C 2 -C 6烯氧基，C 2 -C 6炔氧基，C 1 -C 4烷硫基，芳基，芳氧基或芳硫基，或任选取代的氨基; R 9为羟基，未取代或取代的C 1 -C 10烷基，C 2 -C 6烯基，C 2 -C 6炔基，C 3 -C 8环烷基，芳基或芳氧基，或任选取代的氨基; R 12是氢或未取代的或取代的C 1 -C 10烷基; m为1，3，5，7，9或11; n为0,1或2; X是氟或氯; Y为氢，氟或甲基; 游离形式或盐形式可用作农药，并且可以以本身已知的方式制备。

17. 发明授权

US5783704A Pyridine derivatives as pesticides 失效
标题翻译：吡啶衍生物作为农药
公开(公告)号：US5783704A
公开(公告)日：1998-07-21
申请号：US669452
申请日：1996-06-28
申请人： Henry Szczepanski , Haukur Kristinsson , Peter Maienfisch , Josef Ehrenfreund
发明人： Henry Szczepanski , Haukur Kristinsson , Peter Maienfisch , Josef Ehrenfreund
IPC分类号： A01C20060101 , A01N20060101 , A01N43/40 , A01N43/50 , A01N43/54 , A01N43/653 , A01N43/707 , A01N43/76 , A01N43/78 , A01N43/824 , A01N43/88 , C07D20060101 , C07D253/06 , C07D285/12 , C07D285/13 , C07D401/12 , C07D413/12 , C07D417/12
CPC分类号： C07D253/06 , A01N43/40 , A01N43/50 , A01N43/653 , C07D285/13 , C07D401/12
摘要： Compounds of formu (I) wherein n and Z are as defined in claim 1, and, where appropriate, tautomers thereof, in each case in free form, or in salt form, can be used as agrochemical active ingredients and can be prepared in a manner known per se.
摘要翻译： PCT No.PCT / EP94 / 04222 Sec。 371日期：1996年6月28日 102（e）日期1996年6月28日PCT 1994年12月19日PCT公布。 WO95 / 18123 PCT出版物日期1995年7月6日，其中n和Z如权利要求1中所定义的formu（I）化合物，并且在适当的情况下，其互变异构体以游离形式或盐形式，可用作农业化学活性成分，可以以本身已知的方式制备。

18. 发明授权

US6034083A Pyridine derivatives as pesticides 失效
标题翻译：吡啶衍生物作为农药
公开(公告)号：US6034083A
公开(公告)日：2000-03-07
申请号：US119285
申请日：1998-07-20
申请人： Henry Szczepanski , Haukur Kristinsson , Peter Maienfisch , Josef Ehrenfreund
发明人： Henry Szczepanski , Haukur Kristinsson , Peter Maienfisch , Josef Ehrenfreund
IPC分类号： A01C20060101 , A01N20060101 , A01N43/40 , A01N43/50 , A01N43/54 , A01N43/653 , A01N43/707 , A01N43/76 , A01N43/78 , A01N43/824 , A01N43/88 , C07D20060101 , C07D253/06 , C07D285/12 , C07D285/13 , C07D401/12 , C07D413/12 , C07D417/12 , A61K31/53
CPC分类号： C07D253/06 , A01N43/40 , A01N43/50 , A01N43/653 , C07D285/13 , C07D401/12
摘要： Compounds of formula ##STR1## wherein n and Z are as defined in claim 1, and, where appropriate, tautomers thereof, in each case in free form or in salt form, can be used as agrochemical active ingredients and can be prepared in a manner known per se.
摘要翻译：其中n和Z如权利要求1所定义的化合物，并且在适当的情况下，其互变异构体在每种情况下以游离形式或盐形式可用作农业化学活性成分，并且可以以本身已知的方式制备。

19. 发明授权

US5606057A Process for the preparation of 6-alkyl-4-(pyridin-3-yl-methyleneamino)-4,5-dihydro-1,2,4-triazin-3(2H)- one 失效
标题翻译：制备6-烷基-4-（吡啶-3-基 - 亚甲基氨基）-4,5-二氢-1,2,4-三嗪-3（2H） - 酮的方法
公开(公告)号：US5606057A
公开(公告)日：1997-02-25
申请号：US194183
申请日：1994-02-09
申请人： Thomas Pitterna , Urs Siegrist , Henry Szczepanski
发明人： Thomas Pitterna , Urs Siegrist , Henry Szczepanski
IPC分类号： A01N43/707 , B01J25/02 , C07B61/00 , C07D401/12 , C07D253/06
CPC分类号： C07D401/12
摘要： A process for the preparation of 6-alkyl-4-(pyridin-3-yl-methyleneamino)-4,5-dihydro-1,2,4-triazin-3(2H)-one by the reaction of 4-amino-6-alkyl-3-oxo-2,3,4,5-tetrahydro-1,2,4-triazine with 3-cyanopyridine wherein the reaction is carried out under catalytic hydrogenation conditions in the presence of a Raney-nickel catalyst in an aqueous alcoholic medium, at a temperature between 0.degree. and 70.degree. C., at a pH of between 2 and 7, and in the presence of and a C.sub.1 -C.sub.6 -carboxylic acid or a C.sub.1 -C.sub.6 -carboxylic acid alkali metal salt or both, whereby the hydrogen pressure is between 0.1 and 10 bar.
摘要翻译： 6-氨基-4-（吡啶-3-基 - 亚甲基氨基）-4,5-二氢-1,2,4-三嗪-3（2H） - 酮的制备方法， 6-烷基-3-氧代-2,3,4,5-四氢-1,2,4-三嗪与3-氰基吡啶反应，其中反应在催化氢化条件下在阮内镍催化剂存在下进行水溶性醇介质，温度在0℃至70℃之间，pH为2-7，在C 1 -C 6羧酸或C 1 -C 6羧酸碱金属盐存在下，或两者，由此氢压力在0.1和10巴之间。

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