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    PROCESS FOR THE PREPARATION OF CEPHEM COMPOUNDS
    2.
    发明公开
    PROCESS FOR THE PREPARATION OF CEPHEM COMPOUNDS 有权
    VERFAHREN ZUR HERSTELLUNG VON CEPHEM-VERBINDUNGEN

    公开(公告)号：EP1209160A4

    公开(公告)日：2002-10-30

    申请号：EP00956785

    申请日：2000-08-30

    申请人： OTSUKA KAGAKU KK

    发明人： TANAKA HIDEO ,  KAMEYAMA YUTAKA

    IPC分类号： B01J31/30 ,  C07B61/00 ,  C07D501/00 ,  C07D501/04 ,  C07D501/16 ,  C07D501/22 ,  C07D501/24 ,  C07B37/04 ,  B01J23/755

    CPC分类号： C07D501/00 ,  Y02P20/55

    摘要： A process for the preparation of 3-alkenylcephem or 3-norcephem compounds represented by general formula (3), characterized by treating a 3-cephem compound of general formula (1) in a solvent with an alkenyl halide of general formula (2), a nickel catalyst, a metal having a standard redox potential of -0.3 (V/SCE) or below , and a compound of a metal having a standard redox potential higher than that of the above metal. Formula (1) (wherein R1 is hydrogen or the like; R2 is hydrogen or the like; R3 is hydrogen or a carboxyl-protecting group; and X is halogeno or the like). (Formula 2) R4-Y wherein R4 is optionally substituted 1-alkenyl; and Y is halogeno. Formula (3) (wherein R?1, R2, and R3¿ are each as defined above; and R5 is hydrogen or optionally substituted 1-alkenyl).

    摘要翻译： 1.一种制备式（3）的3-链烯基头孢烯化合物或3-去头孢烯化合物的方法，其特征在于式（2）的烯基卤，镍催化剂，高达-0.3（V / SCE） 在标准氧化还原电位和具有比金属更高的标准氧化还原电位的金属的化合物在溶剂中作用于式（1）的3-头孢烯化合物，其中R 1是 氢原子等，R 2为氢原子等，R 3为氢原子或羧酸保护基，X为卤素原子等，R 4 -Y其中R 4是具有或不具有取代基的1-烯基，Y是卤素原子其中R 1，R 2和R 3如上所定义，R 5是 氢原子或具有或不具有取代基的1-烯基。

    PROCESSES FOR THE PREPARATION OF BETA-LACTAM DERIVATIVE
    3.
    发明公开
    PROCESSES FOR THE PREPARATION OF BETA-LACTAM DERIVATIVE 失效
    METHOD FOR PRODUCTIONβ-内酰胺衍生物的

    公开(公告)号：EP0759436A4

    公开(公告)日：1998-11-25

    申请号：EP96905038

    申请日：1996-03-08

    申请人： OTSUKA KAGAKU KK

    发明人： TORII SIGERU ,  TANAKA HIDEO ,  SASAOKA MICHIO ,  KAMEYAMA YUTAKA ,  WADA ISAO ,  AMANO YASUHISA

    IPC分类号： C07D205/09 ,  C07D205/095 ,  C07D501/00 ,  C07D501/08 ,  C07D513/04 ,  C07D205/08

    CPC分类号： C07D513/04 ,  C07D205/09 ,  C07D205/095 ,  C07D501/00

    摘要： A process for the preparation of an allenyl-β-lactam compound which comprises reacting the hydroxyl group of a β-lactam compound of general formula (1) with a reactive functional derivative of a sulfonic acid of the general formula (2): R5-SO2-X to form a β-lactam compound of general formula (3) and reacting the formed compound with a basic anion-exchange resin containing a tertiary organic base immobilized thereon to attain the preparation of an allenyl-β-lactam compound of general formula (4) and the stable isolation thereof from the reaction mixture in a high yield at a high purity. Another process for the preparation of an allenyl-β-lactam compound which comprises reacting the hydroxyl group of a β-lactam compound of general formula (1) with a reactive functional derivative of a sulfonic acid of the general formula (2): R5-SO2-X to form a β-lactam compound of general formula (3), reacting the formed compound with a tertiary organic base to form an allenyl-β-lactam compound of general formula (4) and treating the resulting reaction mixture with both an acidic cation-exchange resin and a basic anion-exchange resin either alternately or simultaneously to isolate the compound of general formula (4) from the reaction mixture stably. A process of preparing a 3-halocephem derivative of general formula (6) by reacting an allenyl-β-lactam compound of general formula (4) with a halogenating agent in the presence of a sulfinate or thiolate ion scavenger.

    PROCESS FOR THE PREPARATION OF A 3-VINYLCEPHEM COMPOUND
    4.
    发明公开
    PROCESS FOR THE PREPARATION OF A 3-VINYLCEPHEM COMPOUND 有权
    制造方法3乙烯基头孢烯CONNECTION

    公开(公告)号：EP1273587A4

    公开(公告)日：2007-12-26

    申请号：EP01919924

    申请日：2001-04-13

    申请人： OTSUKA KAGAKU KK

    发明人： KAMEYAMA YUTAKA ,  FUKAE KAZUHIRO

    IPC分类号： A61K31/546 ,  A61P31/04 ,  C07D501/00 ,  C07D501/04 ,  C07D501/22

    CPC分类号： C07D501/00

    摘要： A process for the preparation of a 3-vinylcephem compound, characterized by treating a protected 3-vinylcephem derivative of the general formula (1) in an organic solvent in the presence of a perhalogenic acid and an organic protonic acid to thereby obtain a 3-vinylcephem compound of formula (2). In general formula (1), R?1, R2 and R3¿ are each hydrogen or optionally substituted arylmethyl, with the proviso that all of R?1, R2 and R3¿ must not be hydrogen.

    PROCESS FOR PRODUCING BETA-LACTAM DERIVATIVES.
    7.
    发明公开
    PROCESS FOR PRODUCING BETA-LACTAM DERIVATIVES. 失效
    HERSTELLUNGSVERFAHREN VON BETA-LACTAMABKÖMMLINGEN。

    公开(公告)号：EP0222022A4

    公开(公告)日：1987-09-02

    申请号：EP86903558

    申请日：1986-05-17

    申请人： OTSUKA KAGAKU KK

    发明人： SASAOKA MICHIO ,  SAITO NORIO ,  SHIROI TAKASHI ,  NAGAO SHIGEMITSU ,  KIKUCHI RYO ,  KAMEYAMA YUTAKA

    IPC分类号： C07D463/00 ,  C07D498/04 ,  C07D499/00 ,  C07D499/08 ,  C07D501/02 ,  C07D501/04 ,  C07D505/00 ,  C07D471/04

    CPC分类号： C07D505/00 ,  C07D499/00 ,  Y02P20/55

    摘要： A process for producing beta-lactam derivatives, which comprises reacting a beta-lactam derivative wherein the carboxyl group is protected and which is represented by the general formula: A-COO-X (wherein A represents a beta-lactam derivative residue, and X represents a benzyl group having an electron-donating group in the phenyl group, a diphenylmethyl group optionally having an electron-donating group in the phenyl group, or a tert-butyl group) with a phenol to obtain a beta-lactam derivative represented by the general formula: A-COOH (wherein A is the same as defined above).

    摘要翻译： 一种β-内酰胺衍生物的制造方法，其特征在于，使羧基被保护的β-内酰胺衍生物与通式A-COO-X（式中，A表示β-内酰胺衍生物残基，X 表示在苯基中具有供电子基团的苄基，在苯基中任选具有供电子基团的二苯基甲基或叔丁基）与苯酚反应以获得由所述苯基形成的β-内酰胺衍生物 通式：A-COOH（其中A与上述定义相同）。

    PROCESS FOR PRODUCING 3-CEPHEM COMPOUNDS
    8.
    发明公开
    PROCESS FOR PRODUCING 3-CEPHEM COMPOUNDS 有权
    用于生产-3-头孢烷的连接

    公开(公告)号：EP1028118A4

    公开(公告)日：2003-01-22

    申请号：EP98947899

    申请日：1998-10-16

    申请人： OTSUKA KAGAKU KK

    发明人： KAMEYAMA YUTAKA

    IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/00 ,  C07D501/04 ,  C07D501/18 ,  C07D501/26 ,  C07D501/36

    CPC分类号： C07D501/00 ,  Y02P20/55

    摘要： 3-Halogenomethylcephem compounds represented by general formula (2) or salts thereof, produced by reacting a 7-amino-3-halogenomethylcephem compound represented by general formula (1) or a salt thereof with a phenol derivative to remove the 4-position carboxy-protective group; and 3-thiomethylcephem compounds represented by general formula (4) or salts thereof, produced by reacting the 3-halogenomethylcephem compound represented by formula (2) or its salt with either a thiol compound represented by general formula (3): R2S-M or a salt thereof, wherein X?1, R1, R2¿, and M are each as defined in the description.

    PROCESS FOR THE PREPARATION OF 3-CEPHEM COMPOUNDS
    10.
    发明公开
    PROCESS FOR THE PREPARATION OF 3-CEPHEM COMPOUNDS 有权
    用于生产-3-头孢衍生物

    公开(公告)号：EP1010701A4

    公开(公告)日：2001-07-11

    申请号：EP99926869

    申请日：1999-06-30

    申请人： OTSUKA KAGAKU KK

    发明人： KAMEYAMA YUTAKA ,  YAMADA TAKAE ,  SUH DAL SOO

    IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/00 ,  C07D501/04 ,  C07D501/18

    CPC分类号： C07D501/00

    摘要： A process for the preparation of 3-cephem compounds, characterized by reacting a β-lactam compound represented by general formula (1) with a phosphorus halide compound in the presence of an organic base to form an imino-β-lactam compound represented by general formula (2), adding a phenol to the resulting reaction system to conduct alcoholysis simultaneously with the deblocking of the carboxylate ester, and thus obtaining a 3-cephem compound represented by general formula (3) or a salt thereof, wherein R1, R2, R3 and X are each as defined in the description.