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    Process for preparing thiazolino azetidinone and 2-exo-methylenepenam derivative
    1.
    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。

    Process for preparation of azetidinone derivatives
    10.
    发明授权
    Process for preparation of azetidinone derivatives 失效
    氮杂环丁酮衍生物的制备方法

    公开(公告)号：US4798890A

    公开(公告)日：1989-01-17

    申请号：US186693

    申请日：1988-04-21

    申请人： Sigeru Torii ,  Hideo Tanaka ,  Michio Sasaoka ,  Takashi Shiroi

    发明人： Sigeru Torii ,  Hideo Tanaka ,  Michio Sasaoka ,  Takashi Shiroi

    IPC分类号： C07D205/08 ,  C07D205/09 ,  C07D205/095 ,  C07D401/12 ,  C07D417/12 ,  C07B45/00 ,  C07D ,  C07D401/06 ,  C07D403/12

    CPC分类号： C07D205/095 ,  C07D205/09

    摘要： A process for preparing an azetidinone derivative represented by the formula ##STR1## wherein R.sup.1 is hydrogen, halogen or lower alkoxy, R.sup.2 is hydrogen, halogen, lower alkoxy, amino or a group ##STR2## (in which R.sup.5 is substituted or unsubstituted phenyl, substituted or unsubstituted phenylmethyl, substituted or unsubstituted phenoxymethyl, or substituted or unsubstituted benzoyl), or R.sup.1 and R.sup.2, when taken together, are carbonyl, R.sup.3 is substituted or unsubstituted phenyl, and R.sup.4 is hydrogen, optionally substituted hydrocarbon residue or acyl, silyl, sulfonyl or phosphonyl derived from inorganic acid or organic acid, the process comprising reacting a dithioazetidinone derivative represented by the formula ##STR3## wherein R.sup.1, R.sup.2 and R.sup.4 are as defined above and R.sup.9 is substituted or unsubstituted, nitrogen-containing aromatic heterocyclic residue with a compound represented by the formulaR.sup.3 SO.sub.2 H (VII)wherein R.sup.3 is defined above.

    摘要翻译： 制备式（I）表示的氮杂环丁酮衍生物的方法，其中R 1是氢，卤素或低级烷氧基，R 2是氢，卤素，低级烷氧基，氨基或基团（其中R 5是取代的或 未取代的苯基，取代或未取代的苯基甲基，取代或未取代的苯氧基甲基或取代或未取代的苯甲酰基），或R 1和R 2一起为羰基，R 3为取代或未取代的苯基，且R 4为氢，任选取代的烃残基或酰基 ，衍生自无机酸或有机酸的甲硅烷基，磺酰基或膦酰基，该方法包括使由式（VI）表示的二硫代氮杂环丁酮衍生物（其中R 1，R 2和R 4如上所定义）和R 9是取代或未取代的， 含有由式R3SO2H（Ⅶ）表示的化合物，其中R3定义如上的化合物。