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    Process for preparing 2-alpha-methyl-2-beta-(1,2,3-triazol-1-yl)methyl-penam-3-alpha-carboxylic acid derivatives
    3.
    发明公开
    Process for preparing 2-alpha-methyl-2-beta-(1,2,3-triazol-1-yl)methyl-penam-3-alpha-carboxylic acid derivatives 失效
    Verfahren zur Herstellung von 2-α-Methyl-2-β-（1,2,3-三唑-1-基）甲基扑灭-3-α-碳二烯酸酯。

    公开(公告)号：EP0331395A1

    公开(公告)日：1989-09-06

    申请号：EP89301926.5

    申请日：1989-02-27

    申请人： TAIHO PHARMACEUTICAL COMPANY LIMITED ,  OTSUKA KAGAKU KABUSHIKI KAISHA

    发明人： Torii, Sigeru ,  Tanaka, Hideo ,  Tanaka, Motoaki ,  Yamada, Shozo ,  Nakai, Akira

    IPC分类号： C07D499/00 ,  C07D499/44

    CPC分类号： C07D499/00 ,  Y02P20/55

    摘要： 2α-Methyl-2β-(1,2,3-triazol-1-yl)methylpenam-3α-­carboxylic acid derivatives are prepared by reacting a penicillanic acid sulfoxide derivative of the formula
    wherein R is a penicillin carboxyl protecting group, and R₁ is hydrogen or halogen, R₂ is hydrogen, lower alkyl or the like with a triazole derivative of the formula
    wherein R₃ and R₄ are hydrogen, trialkylsilyl, lower alkyl, lower alkoxy or the like and R₅ is hydrogen or silyl substituted with 3 groups selected from the class consisting of lower alkyl, benzyl and phenyl in a solvent.

    摘要翻译： 2α-甲基-2β-（1,2,3-三唑-1-基）甲基亚磺酸-3α-羧酸衍生物通过使式的青霉烷酸亚砜衍生物，其中R是青霉素羧基 R 1为氢或卤素，R 2为氢，低级烷基等与式CHEM的三唑衍生物反应，其中R 3和R 4为氢，三烷基甲硅烷基，低级烷基，低级烷氧基等，R 5为氢 或在溶剂中由选自低级烷基，苄基和苯基的3种基团取代的甲硅烷基。

    Process for preparing 2 beta-substituted-methylpenicillin derivatives
    5.
    发明公开
    Process for preparing 2 beta-substituted-methylpenicillin derivatives 失效
    Verfahren zur Herstellung von 2-beta-substitutionierten-Methyl-penicillinderivaten。

    公开(公告)号：EP0331394A1

    公开(公告)日：1989-09-06

    申请号：EP89301925.7

    申请日：1989-02-27

    申请人： TAIHO PHARMACEUTICAL COMPANY LIMITED ,  OTSUKA KAGAKU KABUSHIKI KAISHA

    发明人： Torii, Sigeru ,  Tanaka, Hideo ,  Tanaka, Motoaki ,  Yamada, Shozo ,  Nakai, Akira

    IPC分类号： C07D499/00

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D499/00 ,  Y02P20/55

    摘要： A process for preparing a 2β-substituted-­methylpenicillin compound of the formula
    wherein -N Y is an optionally substituted heterocyclic group containing 2 to 4 nitrogen atoms as the hetero atom in the ring structure, and R₁ is a penicillin carboxyl protecting group, the process comprising reacting an azetidinonedisulfide compound of the formula
    wherein R₁ is as defined above and R is a substituted or unsubstituted heterocyclic group with a nitrogen-­containing heterocyclic compound of the formula
    wherein
    is as defined above in the presence of a metal compound.

    摘要翻译： 一种制备式CHEM的2β-取代 - 甲基青霉素化合物的方法，其中-NY是含有2-4个氮原子的任选取代的杂环基，作为环结构中的杂原子，R1是青霉素羧基保护基 该方法包括使式的氮杂环丁二烯硫醚化合物（其中R 1如上定义）和R是取代或未取代的杂环基与式CHEM的含氮杂环化合物反应，其中CHEM>如上所定义 在金属化合物的存在下。 ñ

    2Beta-substituted thiomethylpenicillin derivatives and their preparation and use
    8.
    发明公开
    2Beta-substituted thiomethylpenicillin derivatives and their preparation and use 失效
    2-β - 取代的硫代甲基Penizillinderivate和它们的制备和用途。

    公开(公告)号：EP0236074A1

    公开(公告)日：1987-09-09

    申请号：EP87301699.2

    申请日：1987-02-26

    申请人： TAIHO PHARMACEUTICAL COMPANY LIMITED

    发明人： Torii, Sigeru ,  Tanaka, Hideo ,  Tanaka, Motoaki ,  Yamada, Shozo ,  Nakai, Akira ,  Ohbayashi, Hisashi

    IPC分类号： C07D499/00 ,  A61K31/43

    CPC分类号： C07D499/00

    摘要： Disclosed is a penicillin derivative of the formula:
    wherein n is an integer of 0, l or 2; Y is a cyano group, a lower acyl group, a mono- or di-lower alkylthiocarbamoyl group,
    wherein R₁ is a hydrogen atom, a lower alkyl group, a phenyl group, a group -(CH₂) m -OR₂ or -(CH₂) m COOR₂ (m is an integer of l to 6 and R₂ is a hydrogen atom or a penicillin carboxyl ester-forming group which is commonly used for penicillin derivatives) or a phenyl group substituted by at least one member selected from the class consisting of lower alkyl group, halogen atom and lower alkoxy group; and R is a hydrogen atom or a penicillin carboxyl ester-forming group, or a salt thereof. They are useful as β-lactamase inhibitors.

    2beta-substituted-methylpenicillanic acid derivatives, and salts and esters thereof
    9.
    发明公开
    2beta-substituted-methylpenicillanic acid derivatives, and salts and esters thereof 失效
    2-β-取代物甲基青霉烯衍生物和盐酸盐和酯。

    公开(公告)号：EP0272016A1

    公开(公告)日：1988-06-22

    申请号：EP87310583.7

    申请日：1987-12-01

    申请人： TAIHO PHARMACEUTICAL COMPANY LIMITED

    发明人： Torii, Sigeru ,  Tanaka, Hideo ,  Tanaka, Motoaki ,  Yamada, Shozo ,  Nakai, Akira ,  Ohbayashi, Hisashi ,  Ohno, Tomoyasu

    IPC分类号： C07D499/00 ,  A61K31/43

    CPC分类号： C07D499/00 ,  Y02P20/55

    摘要： Disclosed are 2β-substituted-methylpenicillanic acid compounds of the formula
    wherein n is 0, 1 or 2; and -
    is monocyclic or bicyclic heterocyclic ring group which has 2 to 4 nitrogen atoms as hetero atom in its ring structure and which may be optionally substituted with alkyl, alkoxycarbonyl, phenyl, formyl or benzyloxycarbonyl optionally having alkyl, nitro or a halogen atom on the benzene ring, with the proviso that said heterocyclic ring group is not 1,2,3-triazol-1-yl; or salts or esters thereof.
    These compounds are useful as β-lactamase inhibitor.

    摘要翻译： 公开了式CHEM的2个β-取代的 - 甲基青霉烷酸化合物，其中n是0,1或2; 和 - @@@@是在其环结构中具有2至4个氮原子作为杂原子的单环或双环杂环基团，其可任选被烷基，烷氧基羰基，苯基，甲酰基或任选具有烷基，硝基或 所述杂环基团不是1,2,3-三唑-1-基; 或其盐或酯。 这些化合物可用作β-内酰胺酶抑制剂。