cephalosporin antibiotics and procedure for its manufacture

摘要

A cephalosporin antibiotic of the formula:- …CHEM… or a salt or ester thereof,… where R is phenyl, substituted phenyl, cyclohexenyl, cyclohexadienyl, CH3 CH(OH)-, CH3-CH(OSO3H)-, CH3CH(OCH3)-, or an optionally substituted aromatic 5- or 6-membered heterocyclic group containing 1, 2 or 3 heteroatoms each independently selected from O, S and N; R2 is -CH2OCOCH3, -CH2OCONH2, -Cl, -F, -OCH3, -CH2N3, or a group of the formula: …CHEM… where each R3 is independently H or C1-C4 alkyl, m is 1 or 2, n is 3 or 4 and Het is an optionally substituted 5- or 6-membered heterocyclic group containing up to 4 heteroatoms selected from O, S and N, the heterocyclic group being optionally fused to an optionally substituted benzene ring or to a further 5- or 6-membered heterocyclic group containing up to 4 heteroatoms selected from O, S and N; and R1 is a group of the formula -CONR4R5 or -COR6, where either… (a) R4 and R5 are each independently H or C1-C4 alkyl,… (b) R4 is H or C1-C4 alkyl and R5 is an optionally substituted 5 or 6 membered aromatic heterocyclic group containing 1 or 2 nitrogen atoms or… (c) R4 and R5 together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered heterocyclic group containing 1 or 2 N atoms, and R6 is optionally substituted phenyl, or a substituted or unsubstituted optionally benzo-fused 5- or 6-membered heterocyclic group, or the group -CH2NH-C(=NH)(4-pyridyl).