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    • 6. 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。
    • 10. 发明授权
    • Process for preparing cephem compounds
    • 头孢烯化合物的制备方法
    • US5656754A
    • 1997-08-12
    • US211119
    • 1994-03-22
    • Shigeru ToriiHideo TanakaMichio SasaokaTakashi ShiroiYutaka Kameyama
    • Shigeru ToriiHideo TanakaMichio SasaokaTakashi ShiroiYutaka Kameyama
    • B01J27/122C07B61/00C07D205/08C07D205/09C07D205/095C07D501/00C07D501/08C07D501/18C07D501/22C07D501/16
    • C07D205/09C07D205/095C07D501/00Y02P20/55
    • The present invention provides a process for preparing a cephem compound represented by the general formula (3) characterized in that an allenyl-.beta.-lactam compound represented by the general formula (1) is reacted with an organotin compound represented by the general formula (2) in the presence of a monovalent copper salt ##STR1## wherein R.sup.1 is a hydrogen atom, halogen atom, amino or protected amino, R.sup.2 is a hydrogen atom, halogen atom, lower alkoxyl, lower acyl, lower alkyl, lower alkyl having hydroxyl or protected hydroxyl as a substituent, hydroxyl or protected hydroxyl, or R.sup.1 and R.sup.2 form=0 when taken together, R.sup.3 is a hydrogen atom or carboxylic acid protecting group, R.sup.4 is aryl, aryl having a substituent, nitrogen-containing aromatic heterocyclic group or nitrogen-containing aromatic heterocyclic group having a substituent, and m is 0 or 2,(R.sup.5).sub.n --Sn(R.sup.6).sub.4--n (2)wherein R.sup.5 is alkenyl, alkenyl having a substituent, aryl, aryl having a substituent, nitrogen-containing aromatic heterocyclic group or nitrogen-containing aromatic heterocyclic group having a substituent, R.sup.6 is lower alkyl, and n is 1 or 2, ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.5 are the same as defined above.
    • PCT No.PCT / JP93 / 01041 Sec。 371日期:1994年3月22日 102(e)1994年3月22日PCT 1993年7月26日PCT公布。 出版物WO94 / 02490 日期:1994年2月3日本发明提供一种制备由通式(3)表示的头孢烯化合物的方法,其特征在于,将由通式(1)表示的丙烯酰基-β-内酰胺化合物与由 在一价铜盐(1)的存在下通式(2)其中R1是氢原子,卤素原子,氨基或被保护的氨基,R2是氢原子,卤素原子,低级烷氧基,低级酰基, 低级烷基,具有羟基或被保护的羟基作为取代基的低级烷基,羟基或保护的羟基,或者R 1和R 2形成= 0,当R 3是氢原子或羧酸保护基时,R 4是芳基,具有取代基的芳基, 具有取代基的含氮芳香族杂环基或含氮芳香族杂环基,m为0或2,(R5)n-Sn(R6)4-n(2)其中R5为烯基,具有取代基的烯基, ,具有取代基的芳基,氮 - 具有取代基的芳族杂环基或含氮芳族杂环基,R6是低级烷基,n是1或2,其中R1,R2,R3和R5与上述定义相同。