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    • 2. 发明授权
    • Penam derivatives
    • Penam衍生物
    • US5599925A
    • 1997-02-04
    • US314307
    • 1994-09-30
    • Shigeru ToriiHideo TanakaMasatoshi TaniguchiMitio SasaokaTakashi ShiroiYutaka Kameyama
    • Shigeru ToriiHideo TanakaMasatoshi TaniguchiMitio SasaokaTakashi ShiroiYutaka Kameyama
    • C07D499/00C07D499/86C07D499/87C07D499/897
    • C07D499/00Y02P20/55
    • A penam derivative of the general formula ##STR1## wherein R.sup.1 means hydrogen, halogen, amino or protected amino; R.sup.2 means hydrogen, halogen, lower alkoxy, lower acyl, lower alkyl, hydroxy- or protected hydroxy-substituted lower alkyl, hydroxy or protected hydroxy, or R.sup.1 and R.sup.2 may jointly represent oxo; R.sup.3 means hydrogen or a carboxy-protecting group; R.sup.4 means hydrogen; R.sup.5 means a group of the formula --CH.sub.2 Y where Y means halogen, --N.sub.3, --ONO.sub.2, --OR.sup.6, --OCOR.sup.6, --SCSOR.sup.6, --SCSN(R.sup.6).sub.2, --SR.sup.6, --SO.sub.2 R.sup.6, --NHR.sup.6, --N(R.sup.6).sub.2 or a substituted or unsubstituted nitrogen-containing heterocyclic group having a free valence on nitrogen; R.sup.6 means a lower alkyl, aryl or heterocyclic group which is substituted or unsubstituted; or R.sup.4 and R.sup.5 may jointly represent .dbd.CH.sub.2 ; n means 0, 1 or 2; provided, however, that where R.sup.4 and R.sup.5 jointly represent .dbd.CH.sub.2, n is not equal to 0.
    • 其中R 1表示氢,卤素,氨基或被保护的氨基; R 2表示氢,卤素,低级烷氧基,低级酰基,低级烷基,羟基或保护的羟基取代的低级烷基,羟基或保护的羟基,或者R 1和R 2可以共同表示氧代; R3表示氢或羧基保护基; R4表示氢; R5表示式-CH2Y的基团,其中Y表示卤素,-N3,-ONO2,-OR6,-OCOR6,-SCSOR6,-SCSN(R6)2,-SR6,-SO2R6,-NHR6,-N(R6) 2或在氮上具有游离价的取代或未取代的含氮杂环基; R6表示取代或未取代的低级烷基,芳基或杂环基; 或者R4和R5可以共同表示= CH2; n表示0,1或2; 但是,如果R4和R5共同表示= CH2,则n不等于0。