| 摘要 |
NEW MATERIAL:An oxapenam derivative shown by the formula I (R<1> is H or lower alkyl; R<2> is R<1>, lower alkoxycarbonyl, aralkyloxycarbonyl, or COOH; R<3> is aryl; R<4> is R<2> except for COOH), its salt, and a diazoketone compound shown by the formula II. EXAMPLE:2-Phenylthiomethylene-1-oxapenam. USE:An inhibitor of beta-lactamase, antibacterial agent, and its synthetic intermediate. Syergistic effect can be obtained by using the title compound together with an antibiotic of a beta-lactam compound. PROCESS:For example, a compound shown by the formula II is obtained by several processes using a starting material, e.g., a compound shown by the formula III. The compound shown by the formula II is heated in the presence of copper or a cupric salt in a solvent to give a compound shown by a formula I (R<2> is R<5>). An alkali salt of a compound shown by the formula I in the case of R<2>=H is reacted with CO2 to give a compound shown by the formula I in the case of R<2>=COOH. |
