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    NOVEL INTERMEDIATE FOR CARBAPENEM COMPOUND FOR ORAL ADMINISTRATION AND PROCESS FOR PRODUCING THE SAME
    9.
    发明公开
    NOVEL INTERMEDIATE FOR CARBAPENEM COMPOUND FOR ORAL ADMINISTRATION AND PROCESS FOR PRODUCING THE SAME 审中-公开
    新的中间FÜRCARBAPENEMVERBINDUNG口头及其制造方法

    公开(公告)号：EP1582526A4

    公开(公告)日：2008-08-06

    申请号：EP03774004

    申请日：2003-11-13

    申请人： KANEKA CORP

    发明人： NISHINO KEITA ,  KOGA TERUYOSHI

    IPC分类号： C07F9/6561 ,  C07D205/08 ,  C07D477/00 ,  C07D477/04 ,  C07D477/18 ,  C07F7/18 ,  C07F19/00

    CPC分类号： C07F9/65611 ,  C07D205/08 ,  C07D477/18 ,  Y02P20/55

    摘要： A novel intermediate which is for use in efficiently producing a 1β-methylcarbapenem compound for oral administration; and a process for producing the intermediate. The process, which is for producing a novel β-lactam compound represented by the general formula (4), is characterized by reacting a β-lactam compound represented by the general formula (5) as a starting material with a compound represented by the general formula (6) in the presence of a base to obtain a novel β-lactam compound represented by the general formula (1), protecting the hydroxy group, subsequently cyclizing the protected compound in the presence of a strong base, reacting the cyclized compound with diphenylphosphoryl chloride to obtain a novel β-lactam compound represented by the general formula (3), and removing the protective group therefrom. (5) (6) (1) (3) (4) (In the formulae, R1 represents trimethylsilyl or triethylsilyl; R2 represents aryl or heteroaryl; R3 represents C1-10 alkyl or C3-10 cycloalkyl; and X represents halogeno.)

    Azetidinone derivatives useful in the preparation of carbapenem antibiotics
    10.
    发明公开
    Azetidinone derivatives useful in the preparation of carbapenem antibiotics 失效
    Azetidinonderivate zur Herstellung von Carbapenem-Antibiotika

    公开(公告)号：EP0845459A1

    公开(公告)日：1998-06-03

    申请号：EP98103209.7

    申请日：1992-06-01

    申请人： Sankyo Company Limited

    发明人： Hirai, Koichi ,  Iwano, Yuji ,  Koyama, Hiroo ,  Nishi, Takahide ,  Yoshida, Akira ,  Oda, Kozo

    IPC分类号： C07D205/08 ,  C07F7/18 ,  C07D477/04

    CPC分类号： C07D401/12 ,  C07D205/08 ,  C07D403/12 ,  C07D477/04 ,  C07F7/10 ,  C07F7/186 ,  Y02P20/55

    摘要： Compounds of formula (Ia):
    in which: R 1 represents a hydrogen atom or a hydroxy-protecting group; R 2 represents a methyl group; R 3 represents a phenyl group which has a 2-substituent of formula -CYNR 5 R 6 and no further substituent or has one alkyl substituent, wherein Y represents an oxygen or sulphur atom, and R 5 and R 6 are the same or different and each represents an alkyl group, an aryl group, or R 5 and R 6 together with the nitrogen atom to which they are attached form a heterocyclic group; R 4 represents a hydrogen atom or an amino-protecting group; and Z represents a sulphur atom or an oxygen atom,
    are valuable intermediates in the preparation of carbapenem compounds and retain a desirable configuration during conversion to such carbapenem compounds.

    摘要翻译： 式（Ia）化合物：其中：R 1表示氢原子或羟基保护基; R 2表示甲基; R 3表示具有式-CYNR 5 R 6的2-取代基且不具有另外的取代基或具有一个烷基取代基的苯基，其中Y表示氧或硫原子，R 5和 R 6相同或不同，各自表示烷基，芳基或R 5和R 6与它们所连接的氮原子一起形成杂环基; R 4表示氢原子或氨基保护基; Z表示硫原子或氧原子，是制备碳青霉烯化合物的有价值的中间体，并且在转化成这种碳青霉烯化合物期间保持所需的构型。