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    Process for preparing thiazolino azetidinone and 2-exo-methylenepenam derivative
    4.
    发明授权
    Process for preparing thiazolino azetidinone and 2-exo-methylenepenam derivative 失效
    制备噻唑基氮杂环丁酮和2-外 - 亚甲基台am am嗪衍生物的方法

    公开(公告)号：US5288860A

    公开(公告)日：1994-02-22

    申请号：US3024

    申请日：1993-01-11

    申请人： Sigeru Torii ,  Hideo Tanaka ,  Masatoshi Taniguchi ,  Michio Sasaoka ,  Takashi Shiroi ,  Yutaka Kameyama

    发明人： Sigeru Torii ,  Hideo Tanaka ,  Masatoshi Taniguchi ,  Michio Sasaoka ,  Takashi Shiroi ,  Yutaka Kameyama

    IPC分类号： C07D499/00 ,  C07D499/04 ,  C07D499/12 ,  C07D499/87 ,  C07D513/04

    CPC分类号： C07D513/04 ,  C07D499/00 ,  Y02P20/55

    摘要： The present invention provides a thiazolinoazetidinone derivative represented by the formula ##STR1## wherein R.sup.1 is phenyl having or not having substituent(s), methyl having or not having substituent(s) or ##STR2## group, R.sup.3 being phenyl having or not having substituent(s), and R.sup.2 is a hydrogen atom or carboxylic acid protective group, and a process for preparing the same.The present invention further provides a process for preparing a 2-exo-methylenepenam derivative characterized by hydrolyzing the thiazoline ring of a thiazolinoazetidinone derivative of the above formula (1) to effect recyclization and obtain a 2-exo-methylenepenam derivative represented by the formula ##STR3## wherein R.sup.1 and R.sup.2 are as defined above.

    摘要翻译： 本发明提供由式（1）表示的噻唑并氮杂环丁酮衍生物，其中R 1是具有或不具有取代基的苯基，具有或不具有取代基的甲基或基团，R3是具有或不具有取代基的苯基， 不具有取代基，R2为氢原子或羧酸保护基，及其制备方法。 本发明进一步提供了制备2-异亚甲基台内叶酸衍生物的方法，其特征在于水解上述式（1）的噻唑并氮杂环丁酮衍生物的噻唑啉环以进行再循环，得到式（1）所示的2-外 - 亚甲基山梨醇衍生物， 图像（3）其中R1和R2如上所定义。

    Penam derivatives
    8.
    发明授权
    Penam derivatives 失效
    Penam衍生物

    公开(公告)号：US5599925A

    公开(公告)日：1997-02-04

    申请号：US314307

    申请日：1994-09-30

    申请人： Shigeru Torii ,  Hideo Tanaka ,  Masatoshi Taniguchi ,  Mitio Sasaoka ,  Takashi Shiroi ,  Yutaka Kameyama

    发明人： Shigeru Torii ,  Hideo Tanaka ,  Masatoshi Taniguchi ,  Mitio Sasaoka ,  Takashi Shiroi ,  Yutaka Kameyama

    IPC分类号： C07D499/00 ,  C07D499/86 ,  C07D499/87 ,  C07D499/897

    CPC分类号： C07D499/00 ,  Y02P20/55

    摘要： 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.

    摘要翻译： 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。