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    4-Cyano-2-azetidinones and production thereof
    5.
    发明授权
    4-Cyano-2-azetidinones and production thereof 失效
    4-氰基-2-氮杂环丁酮及其制备

    公开(公告)号：US4560508A

    公开(公告)日：1985-12-24

    申请号：US451323

    申请日：1982-12-20

    申请人： Taisuke Matsuo, deceased ,  Michihiko Ochiai ,  Shoji Kishimoto

    发明人： Taisuke Matsuo, deceased ,  Michihiko Ochiai ,  Shoji Kishimoto

    IPC分类号： C07D205/08 ,  C07D205/085 ,  C07D409/14 ,  C07D417/12 ,  C07F7/08 ,  C07F7/10 ,  A61K31/395 ,  C07D401/12 ,  C07D403/12

    CPC分类号： C07D409/14 ,  C07D205/085 ,  C07D417/12 ,  C07F7/0812 ,  C07F7/10

    摘要： 4-Cyano-2-azetidinone derivatives represented by the formula ##STR1## wherein R.sup.1 is an amino group which may be acylated or protected, X is a hydrogen atom or a methoxy group and W is a hydrogen atom or a sulfo group, and methods of producing the same, for example, as represented by ##STR2## wherein R.sup.2 is an acylated or protected amino group, Y is a halogen atom or a group having the formula --OCOR.sup.3, --SCOR.sup.3 or --S(O).sub.n --R.sup.3 (R.sup.3 being a hydrocarbyl group and n an integer 1 or 2), R.sup.4 is an amino group which may be acylated or protected and X is as defined above. Compounds [I] are useful as advantageous intermediates for the synthesis of optically active 4-substituted-2-azetidinone derivatives, and, when W=SO.sub.3 H, [I] are also useful as antimicrobial agents and as beta-lactamase inhibitors.

    摘要翻译： 由下式表示的4-氰基-2-氮杂环丁酮衍生物[Ⅰ]其中R1是可被酰化或保护的氨基，X是氢原子或甲氧基，W是氢原子或磺基 和其制备方法，例如，由如下所示的方法，其中R 2是酰化或保护的氨基，Y是卤素原子或具有式-OCOR 3，-SCOR 3或 - S（O）n -R 3（R 3为烃基，n为整数1或2），R 4为可被酰化或保护的氨基，X如上述定义。 化合物[I]可用作合成光学活性4-取代-2-氮杂环丁酮衍生物的有利中间体，并且当W = SO 3 H时，[I]也可用作抗微生物剂和β-内酰胺酶抑制剂。

    1-carboxymethoxy acetidinones and their production
    7.
    发明授权
    1-carboxymethoxy acetidinones and their production 失效
    1-羧甲氧基乙酸丁酯及其制备

    公开(公告)号：US4794108A

    公开(公告)日：1988-12-27

    申请号：US651033

    申请日：1984-09-14

    申请人： Shoji Kishimoto ,  Michiyuki Sendai ,  Michihiko Ochiai

    发明人： Shoji Kishimoto ,  Michiyuki Sendai ,  Michihiko Ochiai

    IPC分类号： C07D205/085 ,  C07D209/48 ,  C07D403/12 ,  C07D417/12 ,  A61K31/425 ,  C07D205/08 ,  C07D303/48

    CPC分类号： C07D209/48 ,  C07D205/085 ,  C07D403/12 ,  C07D417/12 ,  Y02P20/55

    摘要： A 2-azetidinone derivative having a group of the formula ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each represents a hydrogen atom, alkyl, aryl or arylalkyl which may have a substituent at the 1-position and an amino group, at the 3-position, which may be acylated or protected, its salt or ester, and methods of producing the same, (1) a method comprising subjecting a 2-azetidinone derivative having a group of the formula ##STR2## wherein the symbols are as defined above at the 1-position and an amino group at the 3-position, its salt or ester to an acylation or protective-group introduction reaction, and (2) a method comprising reacting a 2-azetidinone derivative having a hydroxy group at the 1-position and an amino group, at the 3-position, which may be acylated or protected, or its salt with a compound of the formula ##STR3## wherein W is a halogen atom; other symbols are as defined above, its salt or ester. The above objective compounds are utilizable as excellent antimicrobial agents or as valuable intermediates for the synthesis of the same.

    摘要翻译： 具有式“IMAGE”的基团的2-氮杂环丁酮衍生物，其中R 1和R 2相同或不同，并且各自表示可在1位具有取代基的氨基和氢原子的烷基，芳基或芳基烷基， 在可以被酰化或保护的3-位上，其盐或酯及其制备方法，（1）一种方法，包括使具有式“IMAGE”的基团的2-氮杂环丁酮衍生物，其中符号是 如上所述在1-位和3-位上的氨基，其盐或酯进行酰化或保护基导入反应，和（2）包括使具有羟基的2-氮杂环丁酮衍生物在 可以被酰化或保护的3-位上的3-位和氨基，或其与下式的化合物的盐：其中W是卤素原子; 其他符号如上所定义，其盐或酯。 上述目标化合物可用作优异的抗微生物剂或作为其合成的有价值的中间体。