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    ANTIBIOTICS
    5.
    发明专利
    ANTIBIOTICS 未知

    公开(公告)号：CA1048016A

    公开(公告)日：1979-02-06

    申请号：CA293802

    申请日：1977-12-23

    Applicant: GLAXO LAB LTD

    Inventor： COOK MARTIN C ,  GREGORY GORDON I ,  BRADSHAW JANICE

    IPC: C07D501/26

    Abstract: Cephalosporin antibiotics in which the 7.beta.-acylamido group has the structure where R1 is a furyl, thienyl or phenyl group and R2 is a C1-C4 alkyl, C3 -C7 cycloalkyl or phenylgroup except that R2 may not represent a methyl group when R1 represents a furyl group, and in which the 3-position substituent is a carbamoyloxymethyl group possess a particularly valuable combination of properties, exhibiting high antibacterial activity against a broad range of gram positive and gram negative organisms, particularly high stability to .beta.-lactamases produced by various organisms, and stability in vivo. Such compounds include the nontoxic salts, biologically acceptable esters, 1-oxides and solvates of the parent 4-carboxylic acids. The compounds are syn isomers or exist as mixtures of syn and anti isomers containing at least 90% of the syn isomer. The above compounds may be prepared by (a) acylation of the corresponding 7-amino compound or (b) carbamoylation of the corresponding 3-hydroxymethyl compound.

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