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    Pentahalophenyl ester of cyanoacetic acid derivatives
    1.
    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
    3.
    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。