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    Method for removing the protecting group for carboxyl group
    3.
    发明公开
    Method for removing the protecting group for carboxyl group 失效
    Verfahren zur Entfernung derschützendenGruppe von Carboxygruppe。

    公开(公告)号：EP0574940A1

    公开(公告)日：1993-12-22

    申请号：EP93109774.5

    申请日：1993-06-18

    申请人： TANABE SEIYAKU CO., LTD.

    发明人： Kondo, Kazuhiko ,  Horikawa, Hiroshi ,  Iwasaki, Tameo

    IPC分类号： C07D477/00 ,  C07D499/88 ,  C07D498/047 ,  C07D463/00 ,  C07D501/00 ,  C07D498/053

    CPC分类号： C07D501/00 ,  C07D463/06 ,  C07D477/08 ,  C07D499/88 ,  C07D503/00 ,  C07D505/00 ,  Y02P20/55

    摘要： A method for removing substituted or unsubstituted allyl group from β-lactam compound having substituted or unsubstituted allyl group-protecting carboxyl group, which comprises treating said β-lactam compound with palladium catalyst in the presence of allyl-scavenger in aqueous organic solvent, by which the substituted or unsubstituted group can be easily and effectively removed under moderate conditions so that the desired compound can be obtained in high yield at low cost.

    摘要翻译： 一种从具有取代或未取代的烯丙基保护羧基的β-内酰胺化合物中除去取代或未取代的烯丙基的方法，该方法包括在有机溶剂中在烯丙基清除剂存在下，用钯催化剂处理所述β-内酰胺化合物， 取代或未取代的基团可以在中等条件下容易且有效地除去，从而可以低成本高收率地得到所需化合物。

    Novel methods and compounds for the preparation of carbacephems
    4.
    发明公开
    Novel methods and compounds for the preparation of carbacephems 失效
    Verfahren und Verbindungen zur Herstellung von Carbacephemen。

    公开(公告)号：EP0558215A1

    公开(公告)日：1993-09-01

    申请号：EP93301079.5

    申请日：1993-02-15

    申请人： ELI LILLY AND COMPANY

    发明人： Fisher, Jack Wayne ,  Hatfield, Lowell Deloss ,  Hoying, Richard Charles ,  Ray, James Edward

    IPC分类号： C07D413/14 ,  C07D413/04 ,  C07D463/00

    CPC分类号： C07D413/14 ,  C07D413/04 ,  Y02P20/55

    摘要： Compounds and methods as provided for the preparation of carbacephems, useful in producing cephalosporin analogs. The compounds are 4,6 bicyclo compounds characterized by the presence of both an amino protecting chiral auxiliary and a carboxy protecting group. The methods place both protecting groups onto the basic compound structure early in the synthesis scheme and typically retain both throughout, thereby making the overall procedure simple, efficient and high in yield. Removal of the chiral auxiliary and the carboxy protecting group is accomplished with trimethylsilyl iodide to yield the carbacephem nucleus.

    摘要翻译： 提供用于制备碳水化合物的化合物和方法，可用于产生头孢菌素类似物。 该化合物是4,6二环化合物，其特征在于存在氨基保护手性助剂和羧基保护基。 该方法在合成方案的早期将两个保护基团置于碱性化合物结构上，并且通常保留两者，从而使整个方法简单，有效和高产率。 手性助剂和羧基保护基团的去除是用三甲基甲硅烷基碘化物完成的，以产生碳水化合物核。

    Process for preparing doubly blocked 1-carba(1-dethia)-3-cephem-4-carboxylic acids
    6.
    发明公开
    Process for preparing doubly blocked 1-carba(1-dethia)-3-cephem-4-carboxylic acids 失效
    （1-dethia）-3-cephem-4-Carbonsauren。

    公开(公告)号：EP0512813A2

    公开(公告)日：1992-11-11

    申请号：EP92304075.2

    申请日：1992-05-06

    申请人： ELI LILLY AND COMPANY

    发明人： Berglund, Richard Alan

    IPC分类号： C07D463/00

    CPC分类号： C07D463/22

    摘要： A process is provided for producing 7-protected-amino-4-protected carboxy-3-halo-1-carbacephalosporins which includes the steps of mixing the hydrochloride salt of the carbacephalosporin with a polar organic aprotic solvent having a dielectric constant of at least about 20 and a base selected from a group consisting of 5- or 6-membered tertiary cyclic amine containing 0-1 oxygen atoms, and dimethylbenzamine to form the free amine of a carbacephalosporin and thereafter without isolating the free amine mixing it with an acylating agent to result in the doubly blocked carbacephalosporin.

    摘要翻译： 提供了一种制备7-保护氨基-4-保护的羧基-3-卤代-1-碳头孢菌素的方法，包括以下步骤：将碳头孢菌素的盐酸盐与介电常数至少为约 20和选自含有0-1个氧原子的5-或6-元叔环状基团的碱和二甲基苯甲胺以形成碳头孢菌素的游离胺，然后不分离将其与酰化剂混合的游离胺与 导致双重堵塞的碳水化合物。