Preparation of .beta.-lactam-containing antibacterial agents...

Details Preparation of .beta.-lactam-containing antibacterial agents... Preparation of .beta.-lactam-containing antibacterial agents...

C - Chemistry, Metallurgy

07

D

260/111

C07D 499/00 (2006.01) C07D 205/09 (2006.01) C07D 499/88 (2006.01) C07F 9/568 (2006.01)

Patent

CA 1212665

ABSTRACT OF THE DISCLOSURE There is disclosed a process for the preparation of .beta.-lactam-containing compounds of the formula Image where R is hydrogen, lower alkyl, trichloroethyl, acetonyl, benzyl, substituted benzyl, phenyl, substituted phenyl, benzyldryl or a residue that will undergo metabolic activation "in vivo" and have favorable pharmacokinetic properties: R1 is a hydrogen atom, lower alkyl, lower alkoxy, cycloalkyl, or hydroalkyl, with the alcoholic fun- ction of the hydroxy alkyl being free or protected; Z is hydrogen, halogen, hydroxy, amino, carbamoyloxy, mercapto, pyridinium, OR2, OCOR2, NHCOR2, or SR3 wherein each of R2 and R3 is lower alkyl, aryl, or a heterocyclic ring, each of which may be substituted or unsubstituted, and n is 0 or 1. The compounds have wide spectrum antibacterial activity and .beta.-lactamase inhibiting activity.

499579

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