7 METHOXYCEPHALOSPORIN DERIVATIVES THEIR USE AND PREPARATION

摘要

7 alpha -Methoxycephalosporin derivatives of general formula (I): (1) wherein: R1 represents a hydroxy group; a C1-C4 alkoxy group; a C2-C5 aliphatic acyloxy group; a benzoyloxy group which is unsubstituted or has one or more C1-C4 alkyl, C1-C4 alkoxy, nitro or halogen substituents; a benzenesulphonyloxy group which is unsubstituted or has one or more C1-C4 alkyl substituents; or a C1-C3 alkanesulphonyloxy group which is unsubstituted or has one or more C1-C3 alkoxy, cyano, nitro, halogen or C2-C4 alkoxycarbonyl substituents; R2 represents a hydrogen atom, a C1-C4 alkyl group, a halogen atom, a carboxyl group, a C2-C5 alkoxycarbonyl group, a carbamoyl group, an alkylcarbamoyl group in which the alkyl moiety has from 1 to 3 carbon atoms, a di(C1-C3 alkyl)carbamoyl group or a cyano group; R3 represents a hydrogen atom; an acetoxy group; a carbamoyloxy group; or a tetrazolylthio, thiadiazolylthio or oxadiazolylthio group which is unsubstituted or has one or more C1-C3 alkyl, sulphomethyl or di(C1 or C2 alkyl)amino(C1-C3 alkyl) substituents; m is 0 or 1; and n is 0 or 2 exhibit potent antibacterial activity and are thus useful as medicines. The derivatives can be prepared by reacting the corresponding 7 alpha -methoxycephalosporin derivative having an amino group at the 7 beta -position with an acid halide corresponding to the substituted acetyl group which it is desired to attach to the amino group at the 7 beta -position or by reacting Cephamycin C with the same acid halide.