Process for preparing carbapenem derivatives
    22.
    发明公开
    Process for preparing carbapenem derivatives 失效
    Verfahren zur Herstellung von Carbapenem-Derivaten。

    公开(公告)号:EP0582291A1

    公开(公告)日:1994-02-09

    申请号:EP93112499.4

    申请日:1993-08-04

    IPC分类号: C07D477/00

    CPC分类号: C07D477/04

    摘要: Process for preparing carbapenem derivative of the formula [I], which comprises subjecting azetidinone compound of the formula [II] to intramolecular cyclization reaction together with elimination reaction of the group of -SR⁴, followed by re-adding said group of -SR⁴ to the 2-position of the carbapenem skeleton of the intramolecularly cyclized compound, which is industrially useful as process for preparing carbapenem antimicrobials or synthetic intermediate therefor.

    wherein R¹ is protected or unprotected hydroxy-substituted lower alkyl group, R² is hydrogen atom or ester residue, R³ is hydrogen atom or lower alkyl group, and the group of -SR⁴ is group which can be used as substituent at 2-position of the carbapenem antimicrobials.

    摘要翻译: 制备式[I]的碳青霉烯衍生物的方法,其包括将式[II]的氮杂环丁酮化合物与-SR 4的基团的消除反应一起分子内环化反应,然后重新加入所述 - SR <4>分子内环化化合物的碳青霉烯骨架的2-位,其在工业上可用作制备碳青霉烯类抗微生物剂或其合成中间体的方法。 其中R 1为被保护或未被保护的羟基取代的低级烷基,R 2为氢原子或酯残基,R 3为氢原子或低级烷基,-SR 4为 >可以用作碳青霉烯类抗生素的2-位上的取代基。