3-thiazolomethyl cephalosporins as antibiotics
    5.
    发明授权
    3-thiazolomethyl cephalosporins as antibiotics 失效
    3-噻唑甲基头孢菌素作为抗生素

    公开(公告)号:US4665066A

    公开(公告)日:1987-05-12

    申请号:US685676

    申请日:1984-12-24

    CPC分类号: C07D505/00 C07D463/22

    摘要: 7.beta.-[2-(2-Aminothiazol(oxazol)-4-yl)-2-oximinoacetamido]-3-(thiazolium or substituted thiazolium-3-yl)methyl-3-cephem-4-carboxylates and the correspondingly substituted 1-oxadethia and 1-carbadethia 3-cephem compounds are potent antibacterials useful in a therapeutic method for treating bacterial diseases. Also provided are pharmaceutical formulations of these thiazolium-substituted compounds and intermediates useful in the preparation thereof.

    摘要翻译: 7β-[2-(2-氨基噻唑(恶唑)-4-基)-2-肟基乙酰胺基] -3-(噻唑鎓或取代的噻唑鎓-3-基)甲基-3-头孢烯-4-羧酸酯和相应的取代的1 - 恶二唑和1-碳氮烯3-头孢烯化合物是用于治疗细菌性疾病的治疗方法中的有效抗菌剂。 还提供了这些噻唑鎓取代的化合物的药物制剂和可用于其制备的中间体。

    Azetidinone intermediates for 1-carba(dethia)caphalosporins
    10.
    发明授权
    Azetidinone intermediates for 1-carba(dethia)caphalosporins 失效
    氮杂环丁酮中间体,用于1-carba(dethia)caphalosporins

    公开(公告)号:US4885362A

    公开(公告)日:1989-12-05

    申请号:US202287

    申请日:1988-06-06

    IPC分类号: C07D205/085 C07F7/10

    CPC分类号: C07D205/085 C07F7/10

    摘要: Azetidinone-2 intermediates represented by the formula ##STR1## wherein R is phenyl, phenoxy or thienyl, R.sub.1 is --CH.dbd.CH--COOR.sub.1 ' wherein R.sub.1 ' is an ester, e.g., benzyl; --CH.sub.2 CH.sub.2 COR.sub.2 wherein R.sub.2 is OH or imidazol-1-yl; --CH.sub.2 CH.sub.2 C(O)CH.sub.2 COOR.sub.1 ' where R.sub.1 ' is an ester, e.g., p-nitrobenzyl; and R', R" and R'" are C.sub.1 -C.sub.4 alkyl, aryl or aralkyl; are converted to 1-carba(dethia)cephalosporin antibiotics. Preferably, R is phenoxy and the 1-silyl group is dimethyl-t-butylsilyl. Also provided is 3.beta.-phenoxyacetylamino-4.beta.-(2-carboxyethyl)azetidinone, likewise useful in the preparation of 1-carbacephalosporin antibiotics.