| 摘要 |
NEW MATERIAL:A compound shown by the formulaI(R<1> is H, Cl, or Br; R<2> is Cl or Br), its salt and ester. EXAMPLE:2beta-Chloromethyl-2alpha-methylpenam-3alpha-carboxylic acid-1,1-dioxide. USE:An inhibitor for beta-lactamse. The use of it together with a beta-lactam type antibiotic strengthens the antimicrobial activity of the antibiotic. PROCESS:A sulfide shown by the formula II (R<3> is penicillincarboxyl-protecting group) is oxidized with an oxidizing agent such as permanganic acid, periodic acid, etc. in a solvent such as chloroform, pyridine, etc. The reaction product is preferably de-esterified to give a compound shown by the formulaI. If necessary, this compound is subjected to ester exchange reaction or salt-forming reaction, to give an ester hydrolyzable in a living body or a salt pharmaceutically acceptable as a drug. |
