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    Pentahalophenyl ester of cyanoacetic acid derivatives
    3.
    发明授权
    Pentahalophenyl ester of cyanoacetic acid derivatives 失效
    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。

    Process for the preparation of reactive penicillanic acid and cephalosporanic acid derivatives
    4.
    发明授权
    Process for the preparation of reactive penicillanic acid and cephalosporanic acid derivatives 失效
    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。

    Process for the preparation of reactive penicillanic acid and cephalosporanic acid derivatives
    5.
    发明授权
    Process for the preparation of reactive penicillanic acid and cephalosporanic acid derivatives 失效
    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：US4304717A

    公开(公告)日：1981-12-08

    申请号：US36756

    申请日：1979-05-07

    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： C07C69/353 ,  A61K31/43 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D333/24 ,  C07D499/00 ,  C07D499/12 ,  C07D499/72 ,  C07D501/06 ,  C07D501/20 ,  C07D501/22 ,  C07D501/26 ,  C07D501/28 ,  C07D501/32 ,  C07D501/34 ,  C07D501/60

    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 trialkylamine, 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R1是氢或易于除去的形成酯或成盐基团，优选三烷基胺，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为 根据本发明的一组式（IMAGE），式（II）的胺，其中R 4是易于除去的酯形成基团，优选三烷基氨基，三烷基甲硅烷基，三氯乙基，乙酰氧基 乙基，苯甲酰甲基，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。

    Process for the preparation of propargyl amines
    8.
    发明授权
    Process for the preparation of propargyl amines 失效
    炔丙胺的制备方法

    公开(公告)号：US4564706A

    公开(公告)日：1986-01-14

    申请号：US514149

    申请日：1983-07-14

    申请人： Zoltan Ecsery ,  Eva Somfai ,  Judit Hermann nee Voros ,  Lajos Nagy ,  Gabor Szabo ,  Otto Orban ,  Laslzo Arvai

    发明人： Zoltan Ecsery ,  Eva Somfai ,  Judit Hermann nee Voros ,  Lajos Nagy ,  Gabor Szabo ,  Otto Orban ,  Laslzo Arvai

    IPC分类号： C07C67/00 ,  C07C209/00 ,  C07C209/08 ,  C07C211/63 ,  C07C87/28 ,  C07C85/04

    CPC分类号： C07C209/08

    摘要： The invention relates to a new process for the preparation of propargyl ammonium chlorides of the Formula I ##STR1## by alkaline decomposition of the d-tartarate of the 1-isomer of an amine of the Formula II ##STR2## and subsequent reaction of the amine of the Formula II with a halide of the Formula IIIX--CH.sub.2 --C.tbd.CH (III)in the presence of an organic solvent, alkali and waterin which in Formulae II and III respectively,n is 1 or 0 andX stands for halogenwhich comprises reacting the d-tartarate of the 1-isomer of an amine of the Formula II in aqueous suspension with an alkali, dissolving the base of the Formula II, thus set free without isolation in a water non-miscible organic solvent and reacting the same in the said phase with a halide of the Formula III, and thereafter--preferably after separating the aqueous layer--reacting the mixture which contains the amines of the Formulae II and IV ##STR3## in the organic phase in the presence of water with an organic acid or a solution which has a pH value of 1.5-6 and consists of an inorganic acid and water, thus dissolving in the two-phase mixture formed the salt of the amine of the Formula II in the aqueous layer and selectively separating the amine of the Formula II from the amine of the Formula IV, and thereafter adding after the separation of the phases hydrogen chloride to the amine of the Formula IV being in the organic phase and thus precipitating the salt of the Formula I.The compounds of Formula I are known pharmaceutical active ingredients. The advantage of the process of the present invention that it is highly economical and enables the recovery of the starting materials on large scale production too.

    摘要翻译： 本发明涉及通过碱式分解通式II（XIIX）的胺的1-异构体的d-酒石酸来制备式I的炔丙基氯化铵的新方法（I） 和随后的式II的胺与式III的X-CH 2 -C 3 CH 3（III）的卤化物在有机溶剂，碱和水的存在下分别反应，其中式II和III分别为n为1 或0和X表示卤素，其包括使式II的胺的1-异构体在水悬浮液中与碱反应，溶解式II的碱，因此在不分离的情况下在水中非游离 在所述相中与其反应，与式III的卤化物反应，然后优选在将含有式II和IV的胺的混合物（IV）的水层分离成 在有机酸存在下的有机相 或pH值为1.5-6且由无机酸和水组成的溶液，因此溶解在两相混合物中形成水性层中式II的胺的盐，并选择性地分离 式II的式II化合物，然后在将相氯化氢分离为式IV的胺之后加入有机相，由此沉淀式I的盐。式I的化合物是已知的 药用活性成分。 本发明方法的优点是高度经济且能够在大规模生产中回收原料。

    Combined compositions
    10.
    发明授权
    Combined compositions 失效
    组合成分

    公开(公告)号：US5389662A

    公开(公告)日：1995-02-14

    申请号：US687938

    申请日：1991-05-31

    申请人： Laszlo Pap ,  Istvan Szekely ,  Lajos Nagy ,  Andras Szego ,  Andrea Toth ,  Eva Somfai ,  Csaba Szantay ,  Lajos Novak ,  Laszlo Poppe

    发明人： Laszlo Pap ,  Istvan Szekely ,  Lajos Nagy ,  Andras Szego ,  Andrea Toth ,  Eva Somfai ,  Csaba Szantay ,  Lajos Novak ,  Laszlo Poppe

    IPC分类号： A01N43/30 ,  A01N43/50 ,  A01N43/54 ,  A01N43/653 ,  A01N47/38 ,  A01N53/00 ,  A01N53/02 ,  A01N53/04 ,  A01N53/06 ,  A01N53/08 ,  A01N53/14 ,  A01N43/28

    CPC分类号： A01N53/00

    摘要： The invention relates to novel combined compositions for combatting plant, animal and sanitarian as well as forestry, horticultural and warehouse pests. These compositions contain a pyrethroid-type insecticide as an insecticidally active ingredient and at least one fungicide inhibiting the ergosterol biosynthesis as activity-strengthening agent as well as optionally piperonylbutoxide and other additives.The advantages of the compositions according to the invention consist therein that the activity-strengthening substances used are fungicidal agents widely used and have an advantageous toxicology. The activity-strengthening agent exerts a synergistic effect together with the pyrethroid-type insecticide.The combinations according to the invention bear an outstanding importance in the protection of stored crops.

    摘要翻译： PCT No.PCT / HU90 / 00055 Sec。 371日期1991年5月31日 102（e）日1991年5月31日PCT提交1990年7月30日PCT公布。 出版物WO91 / 01640 日期1991年2月21日。本发明涉及用于对抗植物，动物和卫生以及林业，园艺和仓库害虫的新型组合物。 这些组合物含有拟除虫菊酯型杀虫剂作为杀虫活性成分和至少一种抑制麦角甾醇生物合成作为活性增强剂以及任选的胡椒基丁醚和其它添加剂的杀真菌剂。 根据本发明的组合物的优点在于其中使用的活性增强物质是广泛使用的杀真菌剂并且具有有利的毒理学。 活性增强剂与拟除虫菊酯类杀虫剂一起发挥协同作用。 根据本发明的组合在保存作物方面具有突出的重要性。