| 摘要 |
NEW MATERIAL:A compound I (R1 is H, OH, alkoxy, amino, etc.; R2 is alkyl, aralkyl; R3 is alkyl, aryl, aralkyl, alkenyl, alkynyl, etc.; R4 is alkyl, alkenyl, aryl, aralkyl.). EXAMPLE:(4S)-t-butyl-alpha-(4-benzyloxycarbonyl-2-oxoazetidin-1-yl)-al pha-(acetyl) acetamide. USE:beta-Lactamase-inhibiting agent which is expected to be useful as a remedy for infectious diseases by using together with an antibiotic such as penicillin, etc. It is also useful as a synthetic intermediate of a sleleton of beta-lactamase antibiotics. PROCESS:The compound I is prepared by reacting an aspartic acid derivative II with an aldehyde III and an isonitrile IV in an inert solvent at +150--50 deg.C, pref. 0-50 deg.C. |
