Method for producing 6-hydroxyethylpenam compound
    1.
    发明授权
    Method for producing 6-hydroxyethylpenam compound 有权
    6-羟乙基青麻化合物的制备方法

    公开(公告)号:US08293893B2

    公开(公告)日:2012-10-23

    申请号:US12530307

    申请日:2008-03-06

    IPC分类号: C07D499/04 C07D499/861

    摘要: The present invention provides a method by which a 6-hydroxyethyl penam compound represented by General Formula (2) below can be produced with a high selectivity: wherein R represents a hydrogen atom or a protective group for carboxylic acid and X2 represents a halogen atom; the method including the steps of reacting a Grignard reagent with a halogeno penam compound represented by General Formula (1) below: wherein R and X2 are the same as above, and X1 represents a halogen atom; reacting the generated compound with an amine compound; and further reacting the generated compound with acetaldehyde.

    摘要翻译: 本发明提供一种可以高选择性制备下述通式(2)所示的6-羟基乙基青霉烷化合物的方法:其中R表示氢原子或羧酸保护基,X2表示卤素原子; 该方法包括以下步骤:使格利雅试剂与由以下通式(1)表示的卤代双酚化合物反应:其中R和X 2与上述相同,并且X 1表示卤素原子; 使所生成的化合物与胺化合物反应; 并进一步使生成的化合物与乙醛反应。

    Penem derivatives, their preparation and pharmaceutical compositions
containing them
    7.
    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

    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。