2-Oxoazetidine derivatives, their production and use
    4.
    发明公开
    2-Oxoazetidine derivatives, their production and use 失效
    2-Oxoazetidin-Derivate,ihre Herstellung und Verwendung。

    公开(公告)号:EP0053815A1

    公开(公告)日:1982-06-16

    申请号:EP81110154.2

    申请日:1981-12-04

    摘要: 1-Sulfo-2-oxoazetidine derivatives of the general formula (I)
    wherein R 1 is amino group which may optionally be acyiated or protected, X is hydrogen or methoxy, and R 4 is azido, a haiogen, amino group which may optionally be acylated or a group of the formula -OR 5 ,

    or -S-S-R 5 in which R s is an organic residue and n is 0,1 or 2, or a pharmaceutically acceptable salt thereof, or an ester thereof as well as methods of production in accordance with the following schemes:

    wherein R 2 is an acylated or protected amino group, R 3 is an acylated amino group, and R 1 and R 4 are as above defined. The compounds [I] have antimicrobial and β-lactamase inhibitory activity.

    摘要翻译: 通式(I)的1-磺基-2-氧代氮杂环丁啶衍生物... 其中R 1是任选被酰基或保护的氨基,X是氢或甲氧基,R 4是叠氮基,卤素,氨基, 可以任选地被酰化或者其中R 5是有机残基且n是0,1或2,或其药学上可接受的盐或其酯的式-OR 5,... CH 2或-SS-R 5的基团 以及根据以下方案的生产方法:... 其中R2是酰化或保护的氨基,R3是酰化氨基,R1和R4如上所定义。 化合物[I]具有抗微生物和β-内酰胺酶抑制活性。

    Method of preparing 1-sulfo-2-oxoazetidine derivatives and intermediates therefor
    6.
    发明公开
    Method of preparing 1-sulfo-2-oxoazetidine derivatives and intermediates therefor 失效
    Verfahren zur Herstellung von 1-Sulfo-2-oxoazetidin-Derivaten und die Zwischenprodukte。

    公开(公告)号:EP0053387A1

    公开(公告)日:1982-06-09

    申请号:EP81110039.5

    申请日:1981-12-01

    摘要: 1-Sulfo-2-oxoazetidine derivatives represented by the formula (I)
    wherein R, stands for an amino group which may optionally be acylated or protected, and X stands for hydrogen or methoxy, is produced by subjected a 1-t-butyl or isopropylsilyl derivative of a compound represented by the formula (II)
    wherein R 2 stands for an amino group which is acylated or protected, and X is of the same meaning as defined above, to sulfonation, followed by, when R 2 is a protected amino group, removing the protective group, if necessary.
    The compounds represented by the formula (I) have an excellent antibacterial and β-lactamase-inhibitory activity, thus being useful as drugs for humans and domestic animals.

    摘要翻译: 由式(I)表示的1-磺基-2-氧代氮杂环丁烷衍生物其中R1代表任选被酰化或保护的氨基,X代表氢或甲氧基,是通过使1-t- 式(II)表示的化合物的丁基或异丙基甲硅烷基衍生物其中R2表示被酰化或保护的氨基,X与上述定义相同,表示磺酸化,其后,当R 2为 被保护的氨基,必要时除去保护基。 由式(I)表示的化合物具有优异的抗细菌和β-内酰胺酶抑制活性,因此可用作人和家畜的药物。