| 摘要 |
NEW MATERIAL:The compound of formulaI(R is methyl or phenyl). EXAMPLE:Penicillanic acid-1,1-dioxide (5-methyl-2-oxo-1,3-dioxolen-4-yl)-methyl ester. USE:A beta-lactamase inhibiting agent exhibiting excellent absorbability or bioavailability in living body by oral administration. PROCESS:The compound of formulaIcan be prepared by reacting the penicillanic acid-1,1-dioxide of formula II or its salt with the compound of formula III (X is halogen) in an inert organic solvent such as DMF preferably in the presence of a base (e.g. NaHCO3) at -40-+80 deg.C, preferably -10 deg.C- room temperature. The compound of formula III used as a starting raw material is a novel compound, and is obtained by the reaction of the compound of formula IV with a halogenating agent (e.g. N-bromosuccinimide). |
