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12 条记录 (耗时 0.018 秒)

    Penem derivatives, their preparation and pharmaceutical compositions containing them
    1.
    发明授权
    Penem derivatives, their preparation and pharmaceutical compositions containing them 失效
    Penem衍生物，它们的制备和含有它们的药物组合物

    公开(公告)号：US5747483A

    公开(公告)日：1998-05-05

    申请号：US414081

    申请日：1995-03-17

    申请人： Maria Altamura ,  Federico Maria Arcamone ,  Enzo Perrotta ,  Vittorio Pestellini ,  Piero Sbraci ,  Giuseppe Cascio

    发明人： Maria Altamura ,  Federico Maria Arcamone ,  Enzo Perrotta ,  Vittorio Pestellini ,  Piero Sbraci ,  Giuseppe Cascio

    IPC分类号： C07D499/88 ,  A61K31/43 ,  A61K31/48 ,  A61P31/04 ,  C07D499/883 ,  C07D499/897 ,  C07D499/861

    CPC分类号： C07D499/88

    摘要： Penem derivatives of general formula (I), below, and pharmaceutically acceptable salts thereof are disclosed. ##STR1## wherein: R.sub.1 is H, C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.7 cycloalkyl, or an optionally protected C.sub.1 -C.sub.6 hydroxyalkyl; R.sub.2 is a free or esterified carboxyl group or a carboxylate anion; R.sub.3 is H or C.sub.1 -C.sub.6 alkyl; R.sub.4 is H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.1 -C.sub.6 mercaptoalkyl, C.sub.1 -C.sub.6 aminoalkyl, C.sub.1 -C.sub.6 alkyl substituted by a quaternary ammonium group, C.sub.1 -C.sub.6 carboxyalkyl, cycloalkyl, aryl, arylalkyl, heterocyclyl-alkyl optionally substituted, saturated or unsaturated heterocycle, or R.sub.3 and R.sub.4 are linked together to form a heterocyclic ring having 3-7 atoms; R.sub.5 and R.sub.6 independently are H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.1 -C.sub.6 mercaptoalkyl, C.sub. -C.sub.6 aminoalkyl, alkenyl, cycloalkyl, aryl, arylalkyl, alkylaryl, heterocyclyl-alkyl, C.sub.1 -C.sub.6 alkyl carboxyamide, or R.sub.5 and R.sub.6 are taken together to form a heterocyclic ring having 3-7 atoms, and n is an intiger from 1 to 3.

    摘要翻译： 公开了下述通式（I）的苦味衍生物及其药学上可接受的盐。 （I）其中：R 1是H，C 1 -C 6烷氧基，C 3 -C 7环烷基或任选保护的C 1 -C 6羟烷基; R2是游离的或酯化的羧基或羧酸根阴离子; R3是H或C1-C6烷基; R4是H，C1-C6烷基，C1-C6羟基烷基，C1-C6巯基烷基，C1-C6氨基烷基，被季铵基团取代的C1-C6烷基，C1-C6羧基烷基，环烷基，芳基，芳基烷基， 取代的饱和或不饱和杂环，或者R 3和R 4连接在一起形成具有3-7个原子的杂环; R5和R6独立地是H，C1-C6烷基，C1-C6羟基烷基，C1-C6巯基烷基，C-C6氨基烷基，烯基，环烷基，芳基，芳基烷基，烷基芳基，杂环基 - 烷基，C1-C6烷基羧酰胺或R5和 R6一起形成具有3-7个原子的杂环，并且n是1至3的酸酐。

    Process for the preparation of 2-halomethyl-penems and their use for the preparation of antibacterial penems
    3.
    发明授权
    Process for the preparation of 2-halomethyl-penems and their use for the preparation of antibacterial penems 失效
    制备2-卤代甲基青铜的方法及其用于制备抗菌青铜的方法

    公开(公告)号：US6153747A

    公开(公告)日：2000-11-28

    申请号：US130264

    申请日：1998-08-06

    申请人： Enzo Perrotta ,  Maria Altamura

    发明人： Enzo Perrotta ,  Maria Altamura

    IPC分类号： C07D499/883 ,  C07D205/09 ,  C07D499/88 ,  C07D499/887

    CPC分类号： C07D499/88 ,  C07D205/09 ,  Y02P20/55

    摘要： Process for the preparation of 2-halomethyl-penems (I) comprising (a) reacting an acetoxy-(protected hydroxyethyl)-2-azetidinone (III) with a 2-halothioacetic acid to form a 3-haloacetylthioazetidinone (V), (b) reacting (V) with oxalyl chloride to give an intermediate (VII), acylated on the beta-lactamic nitrogen, and (c) cyclizing (VII) in the presence of an organic phosphate or phosphonite to produce the corresponding 2-halomethyl-penem (I).

    摘要翻译： （I）的制备方法，包括（a）使乙酰氧基 - （被保护的羟乙基）-2-氮杂环丁酮（III）与2-卤代硫代乙酸反应以形成3-卤代乙酰基硫代氮杂环丁酮（V），（b） ）使（V）与草酰氯反应得到在β-内酰胺氮上酰化的中间体（VII），和（c）在有机磷酸盐或亚膦酸盐存在下环化（VII）以产生相应的2-卤代甲基 - （一世）。

    Oxidation process for preparing 4-acyloxy azetidinones in a two-phase system
    8.
    发明授权
    Oxidation process for preparing 4-acyloxy azetidinones in a two-phase system 失效
    在两相体系中制备4-酰氧基氮杂环丁酮的氧化方法

    公开(公告)号：US5043440A

    公开(公告)日：1991-08-27

    申请号：US107050

    申请日：1987-10-13

    申请人： Marco Ricci ,  Maria Altamura ,  Daniele Bianchi ,  Walter Cabri ,  Norberto Gatti

    发明人： Marco Ricci ,  Maria Altamura ,  Daniele Bianchi ,  Walter Cabri ,  Norberto Gatti

    IPC分类号： A61K31/397 ,  A61P31/04 ,  C07D205/08

    CPC分类号： C07D205/08 ,  Y02P20/55

    摘要： Process for preparing compounds according to formula (I) ##STR1## wherein R.sub.1 and R.sub.2 represent a hydrogen atom or a protective group and R.sub.3 represents a C.sub.1 -C.sub.10 alkyl or an aryl group, by oxidation of compounds according to formula (II) ##STR2## wherein R.sub.1, R.sub.2 and R.sub.3 have the above-mentioned meanings, in a two-phase system comprising:a) an organic phase including a 4-acylazetidinone compound (II) and an "onium" salt dissolved in a medium immiscible with water,b) an aqueous solution including an alkali or alkaline-earth metal salt of an organic or inorganic peracid.4-Acyloxyazetidinones (I) are useful intermediates in the synthesis of anti-bacterial compounds.

    摘要翻译： 制备式（I）化合物的方法其中R 1和R 2表示氢原子或保护基，R 3表示C 1 -C 10烷基或芳基，通过式（II）化合物的氧化 ）其中R1，R2和R3具有上述含义，在两相体系中，包括：a）包含4-酰基氮杂环丁酮化合物（II）和溶于 与水不混溶的介质，b）包含有机或无机过酸的碱金属或碱土金属盐的水溶液。 4-酰氧基氮杂环丁酮（I）是合成抗菌化合物的有用中间体。