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31. 发明授权

US5338868A Process for preparing alpha-amino-phenylacetic acid-trifluoromethane sulfonic acid mixed anhydrides 失效
标题翻译： α-氨基 - 苯乙酸 - 三氟甲磺酸混合酸酐的制备方法
公开(公告)号：US5338868A
公开(公告)日：1994-08-16
申请号：US689828
申请日：1991-05-24
申请人： Karoly Ban , Annamaria Ban , Lajosne Pali , Marta Kruppa , Eva Somfai , Csaba Huszar
发明人： Karoly Ban , Annamaria Ban , Lajosne Pali , Marta Kruppa , Eva Somfai , Csaba Huszar
IPC分类号： C07C227/18 , C07C229/36 , C07C309/00 , C07D307/58 , C07D305/12 , C07C229/00
CPC分类号： C07D307/58 , C07C227/18 , C07C229/36 , C07C309/00
摘要： A process is disclosed for the preparation of a compound of the Formula (VI) ##STR1## wherein X is a hydrogen atom, or OH,Y is a hydrogen atom, OH or a methyl group,R.sup.2 is a CH--COOR group, or a group of the formula (XI) ##STR2## and R is a C.sub.1 to C.sub.2 alkyl group, which comprises the step of: reacting a condensed salt of the Formula (IV) ##STR3## wherein Me is Na.sup.+ or K.sup.+, with a reactive derivative of trifluoromethane-sulfonic acid of the Formula (V)F.sub.3 C--SO.sub.2 OH.The compounds of the Formula (VI) are intermediates in the preparation of penicillins and cephalosporins with antibiotic activity.
摘要翻译：公开了制备式（VI）化合物（VI）的方法，其中X是氢原子，或OH，Y是氢原子，OH或甲基，R2是CH-COOR 基团或式（XI）的基团（XI），R是C1至C2烷基，其包括以下步骤：使式（IV）的缩合盐与其中 Me是Na +或K +，其具有式（V）F3C-SO 2 OH的三氟甲磺酸的反应性衍生物。式（VI）的化合物是制备具有抗生素活性的青霉素和头孢菌素的中间体。

32. 发明授权

US5153349A Process for the preparation of cypermethrine isomers 失效
标题翻译：制备CYPERMETHRINE异构体的方法
公开(公告)号：US5153349A
公开(公告)日：1992-10-06
申请号：US601767
申请日：1990-10-19
申请人： Sandor Zoltan , Gyorgy Hidasi , Bela Bertok , Istavan Szekely , Janis Hajimichael , Sandor Botar , Lajos Nagy , Eva Somfai , Istvan Lak , Andras Rapi , Antal Gajary , Agnes Hegedus , Maria Tary
发明人： Sandor Zoltan , Gyorgy Hidasi , Bela Bertok , Istavan Szekely , Janis Hajimichael , Sandor Botar , Lajos Nagy , Eva Somfai , Istvan Lak , Andras Rapi , Antal Gajary , Agnes Hegedus , Maria Tary
IPC分类号： A01N53/00 , C07C255/14
CPC分类号： A01N53/00
摘要： The invention relates to a process for the preparation of such isomer mixtures of cypermethrine of the Formula (I) ##STR1## wherein carbon atoms indicated by 1, 3 and .alpha. stand for a chiral carbon atom and the wavy line indicates cis or trans configuration related to the cyclopropane ring--which contains out of the theoretically possible 8-isomers of cypermethrine at least 95% of 1RtransS and 1StransR (Ib) isomer pair or only a mixture of 1RcisC and 1ScisR (Ia) and the isomer pair (Ib) of the ratio (Ia):(Ib)=55:45-25:75 by asymmetric transformation of second order performed in the presence of an amine base and solvent from a starting cypermethrine isomer mixture which contains next to the isomer pair (Ib) cis and other trans isomers or the isomer pair Ia+Ib at an undesired ratio.
摘要翻译： PCT No.PCT / HU90 / 00006 Sec。 371 1990年10月19日第 102（e）1990年10月19日PCT PCT 1990年1月17日PCT公布。出版物WO90 / 08132 日本1990年7月26日。本发明涉及一种制备式（I）的氯氰菊酯的异构体混合物的方法，其中由1,3和α表示的碳原子代表手性碳原子并且波浪线表示与环丙烷环有关的顺式或反式构型，其中含有理论上可能的氯氰菊酯的8-异构体至少95％的1RtransS和1StransR（Ib）异构体对，或仅包含1RcisC和1ScisR（Ia ）和通过在胺碱和溶剂的存在下由起始氯氰菊酯异构体混合物进行的二级的不对称转化，比率（Ia）：（Ib）= 55:45-25:75的异构体对（Ib）= 55：45-25：异构体对（Ib）顺式和其他反式异构体或异构体对Ia + Ib处于不期望的比例。

33. 发明授权

US4508658A Pentahalophenyl ester of cyanoacetic acid derivatives 失效
标题翻译：氰乙酸衍生物的五氢苯基酯
公开(公告)号：US4508658A
公开(公告)日：1985-04-02
申请号：US113380
申请日：1980-01-18
申请人： Magda Huhn , Gabor Szabo , Peter Dvortsak , Marianna Karpati , Eva Somfai
发明人： Magda Huhn , Gabor Szabo , Peter Dvortsak , Marianna Karpati , Eva Somfai
IPC分类号： C07C255/41 , C07C67/00 , C07C253/00 , C07C253/30 , C07C255/19 , C07C255/32 , C07D213/26 , C07D213/57 , C07D307/38 , C07D333/12 , C07D333/24 , C07C121/46
CPC分类号： C07C255/00
摘要： Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or C.sub.1 to C.sub.6 alkyl;R.sup.2 is hydrogen, phenyl, thienyl, furyl, pyridyl, C.sub.1 to C.sub.6 alkyl, furylalkyl where the alkyl is C.sub.1 to C.sub.6, or phenylalkyl where the alkyl is C.sub.1 to C.sub.6 ; orR.sup.1 and R.sup.2 together form C.sub.1 to C.sub.4 alkylene, furyl-C.sub.1 to C.sub.4 alkylene or phenyl-C.sub.1 to C.sub.4 alkylene; and X is halo; ora pharmaceutically acceptable salt thereof, are disclosed as well as a process for the preparation thereof. The new compounds are intermediates useful in the production of penicillins and cephalosporins with antibiotic activity.
摘要翻译：式IMA的化合物，其中R 1是氢或C 1 -C 6烷基; R2是氢，苯基，噻吩基，呋喃基，吡啶基，C1至C6烷基，其中烷基为C1至C6的呋喃基烷基，或烷基为C1至C6的苯基烷基; 或R 1和R 2一起形成C 1至C 4亚烷基，呋喃基-C 1至C 4亚烷基或苯基-C 1至C 4亚烷基; 且X为卤素; 或其药学上可接受的盐，以及其制备方法。新化合物是可用于生产具有抗生素活性的青霉素和头孢菌素的中间体。

34. 发明授权

US4419524A Process for the preparation of dihalovinylcyclopropanecarboxylic acids 失效
标题翻译：二卤乙烯基环丙烷羧酸的制备方法
公开(公告)号：US4419524A
公开(公告)日：1983-12-06
申请号：US350424
申请日：1982-02-19
申请人： Ferenc Lindwurm , Jozsef Muskovits , Sandor Zoltan , Rezso Kolta , Rudolf Soos , Tivadar Puskas , Eva Somfai , Gyorgy Hidasi
发明人： Ferenc Lindwurm , Jozsef Muskovits , Sandor Zoltan , Rezso Kolta , Rudolf Soos , Tivadar Puskas , Eva Somfai , Gyorgy Hidasi
IPC分类号： C07C61/40 , B01J31/02 , C07B61/00 , C07C27/02 , C07C51/00 , C07C51/09 , C07C67/00 , C07C69/743
CPC分类号： C07C51/09
摘要： The invention relates to a new process for the preparation of cyclopropanecarboxylic acids of the formula (I) ##STR1## wherein X and Y independently stand for halogen, by the alkaline hydrolysis of the corresponding alkyl esters having 1 to 6 carbon atoms in the alkyl moiety, in or without a water-miscible organic solvent, in the presence of a phase transfer catalyst. The hydrolysis is carried out with a 2 to 50% by weight aqueous alkali hydroxide solution. If desired, under suitable conditions the cis/trans ratio of the original ester can be altered in the end products. The cyclopropanecarboxylic acids of the formula (I) are obtained in a high purity and are useful intermediates of insecticidally active pyrethroids.
摘要翻译：本发明涉及一种制备式（I）的环丙烷羧酸的新方法，其中X和Y独立地代表卤素，通过碱性水解相应的具有1-6个碳原子的烷基酯在烷基部分，在或不与水混溶的有机溶剂中，在相转移催化剂的存在下。水解用2至50重量％的碱金属氢氧化物水溶液进行。如果需要，在合适的条件下，可以在最终产物中改变原始酯的顺式/反式比。式（I）的环丙烷羧酸以高纯度获得，是杀虫活性拟除虫菊酯的有用中间体。

35. 发明授权

US4171303A Process for the preparation of reactive penicillanic acid and cephalosporanic acid derivatives 失效
标题翻译：反应性青霉烷酸和头孢烷酸衍生物的制备方法
公开(公告)号：US4171303A
公开(公告)日：1979-10-16
申请号：US812735
申请日：1977-07-05
申请人： Magda Huhn , Gabor Szabo , Gabor Resofszki , Eva Somfai
发明人： Magda Huhn , Gabor Szabo , Gabor Resofszki , Eva Somfai
IPC分类号： C07D499/00 , C07D499/72 , C07D501/06 , C07D499/04 , C07D501/04
CPC分类号： C07D499/00
摘要： This invention relates to a process for the preparation of acid amides having the formula (I) or their salts ##STR1## wherein R.sup.1 is hydrogen or an easily removable ester-forming or salt-forming group, preferably a trialkylamino, trialkylsilyl, trichloroethyl, acetoxymethyl, phenacyl, substituted phenacyl, substituted phenyl or benzyl group,R.sup.2 is hydrogen, alkyl group, alkenyl group, alkyl group having an aryl or heterocyclic (preferably furyl or thienyl)-substituent, an aryl group having an alkyl substituent (preferably xylyl), or an aryl, aralkyl or heterocyclic group, (preferably a phenyl, thienyl, or furyl group) which can have one or more substituents,R.sup.3 is hydrogen, or substituted or unsubstituted aryl, alkyl, cycloalkyl or aralkyl group, andX is a group of one of the formulae ##STR2## according to the invention an amine of the formula (II), ##STR3## wherein R.sup.4 is an easily removable ester-forming group, preferably a trialkylamino, trialkylsilyl, trichloroethyl, acetoxymethyl, phenacyl, substituted phenacyl, substituted phenyl or benzyl group, or a salt formed preferably with an alkali metal or a trialkylamine, is acylated with an ester of the formula (III), ##STR4## wherein R.sup.5 is a substituted or unsubstituted aryl, alkyl, cycloalkyl or aralkyl group, and, if desired, substituents R.sup.4 and/or R.sup.5 of the obtained product can be split off, and/or, if desired, the obtained product is converted into its salt or a salt is converted into the free acid.
摘要翻译：本发明涉及一种制备具有式（I）的酸酰胺或其盐（I）的方法，其中R 1是氢或易于除去的形成酯或成盐基团，优选三烷基氨基，三烷基甲硅烷基，三氯乙基，乙酰氧基甲基，苯甲酰甲基，取代的苯甲酰甲基，取代的苯基或苄基，R2是氢，烷基，烯基，具有芳基或杂环（优选呋喃基或噻吩基） - 取代基的烷基，具有烷基取代基的芳基二甲苯基）或可具有一个或多个取代基的芳基，芳烷基或杂环基（优选苯基，噻吩基或呋喃基），R 3为氢或取代或未取代的芳基，烷基，环烷基或芳烷基，X 是根据本发明的一种式（II）的式（II）的胺，其中R 4是易于除去的成酯基团，优选三烷基氨基，三烷基甲硅烷基，三氯乙基，乙酰氧基取代的苯甲酰甲基，取代的苯基或苄基，或优选与碱金属或三烷基胺形成的盐，用式（III）的酯，其中R5是取代或未取代的芳基，烷基，环烷基或芳烷基，并且如果需要，所得产物的取代基R 4和/或R 5可以被分离，和/或如果需要，将得到的产物转化为其盐或盐被转化进入游离酸。

36. 发明授权

US4162327A N,N-Disubstituted-2-furylethyl amines 失效
标题翻译： N，N-二取代-2-呋喃乙基胺
公开(公告)号：US4162327A
公开(公告)日：1979-07-24
申请号：US754278
申请日：1976-12-27
申请人： Jozsef Knoll , Zoltan Ecsery , Judit Hermann nee Voros , Zoltan Torok , Eva Somfai , Gabor Bernath
发明人： Jozsef Knoll , Zoltan Ecsery , Judit Hermann nee Voros , Zoltan Torok , Eva Somfai , Gabor Bernath
IPC分类号： C07D307/52 , A61K31/34
CPC分类号： C07D307/52
摘要： A compound of the formula ##STR1## or a pharmaceutically effective salt thereof in which R.sup.1 and R.sup.2 are hydrogen or lower alkyl and R.sup.3 is halogenoalkenyl or propinyl. The compounds have pharmacological effects similar to those of phenylethylamine but are free from the amphetamine effect with an excellent therapeutic index and selectivity especially with respect to inhibition of monoaminooxidase.
摘要翻译：其中R 1和R 2为氢或低级烷基且R 3为卤代烯基或丙烯基的式IMA化合物或其药学上有效的盐。该化合物具有与苯乙胺类似的药理作用，但是没有苯丙胺作用，具有优异的治疗指数和选择性，特别是在抑制单氨基氧化酶方面。

37. 发明授权

US3964894A Method of controlling plant growth 失效
标题翻译：控制植物生长的方法
公开(公告)号：US3964894A
公开(公告)日：1976-06-22
申请号：US458999
申请日：1974-04-08
申请人： Geza Toth , Gabor Szabo , Gyorgy Eibel , Eva Somfai
发明人： Geza Toth , Gabor Szabo , Gyorgy Eibel , Eva Somfai
IPC分类号： A01N43/38 , C07D417/06 , A01N9/22
CPC分类号： C07D417/06 , A01N43/38
摘要： A method of controlling plant growth wherein the plant or its seed are treated with thiazolyl-indolyl compounds.
摘要翻译：一种控制植物生长的方法，其中用噻唑基 - 吲哚基化合物处理植物或其种子。

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