NOVEL 1-OXA-1-DETHIA-CEPHALOSPORIN DERIVATIVE

摘要

NEW MATERIAL:The compound of formula I {R is group of formula II (R1 is 2- or 3-thienyl; R2 is H or carboxy) or formula III [R3 is H or (carboxy)-lower alkyl]; R4 is H or methoxy; R5 is lower alkyl; R6 is group of formula IV [Het is (substituted) heterocyclic group]}. EXAMPLE:7-( 2-Thienylacetamido )-2alpha-methyl-4-( 1-methyl-1H-tetrazol-5-yl )-thiomethyl-1-oxa-1-dethia-3-cephem-4-carboxylic acid. USE:Antibacterial agent. Antibiotic substance useful for the remedy and prevention of bacterial infectious diseases. PROCESS:The objective compound can be prepared by condensing the compound of formula V (A is carboxyl-protecting group) with a carboxylic acid (or its reactive derivative) in an organic solvent (e.g. methylene chloride), and eliminating the protecting group e.g. with an acid. The compound of formula V is a novel substance, which can be synthesized e.g. from the compound of formula VIvia several steps.