1-oxadethiacephalosporin derivatives and the production thereof

Details 1-oxadethiacephalosporin derivatives and the production thereof 1-oxadethiacephalosporin derivatives and the production thereof

C - Chemistry, Metallurgy

07

D

260/244.2

C07D 498/04 (2006.01) C07D 505/00 (2006.01)

Patent

CA 1148949

TITLE OF INVENTION New 1-oxadethiacephalosporin derivatives and the production thereof ABSTRACT OF THE DISCLOSURE New antibacterial 1-oxadethiacephalosporin derivatives of the genaral formula Image wherein R is a heterocyclic group or a group -S-Het where Het denotes a heterocyclic group, Y is a hydrogen atom or a methoxy group; x and y are each an integer of 1 to 3 is produced by a process comprising condensing a l-oxacephem compound of the formula Image wherein R, Y, y are as defined above; R' is a hydrogen atom or a carboxyl-protecting group; and Z is a halo group, with a sulfur-containing amino acid of the formula Image wherein x is as defined above,in a solvent and removing, - 2 - if necessary, the residual protective group from the resultant condensation product. The new l-oxadethiacephalo- sporin derivatives and the pharmaceutically acceptable salts and esters thereof exhibit high and broad "in vitro" and "in vivo" antibacterial activity, particularly against .beta.-lactamase-producing strains of gram-negative bacteria.

363652

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