申请人:ELI LILLY AND COMPANY
公开号:EP0060119A1
公开(公告)日:1982-09-15
4-Fluoroazetidinones of formula 1
wherein R is a carboxy-substituted or esterified carboxy-substituted butenyl group represented by the formulas
and R1 is amino, amido, imido or imidazolidino or a pharmaceutically-acceptable salt thereof obtained from penicillin are useful intermediates in the preparation of β-lactam antibiotics. 4-Fluoroazetidinones of formula 1 wherein R1 as described above other than amino, benzyloxycarbonylamino, p-nitrobenzyloxycarbonylamino, t-butyloxycarbonylamino, 2,2,2-tnchloroethoxycarbonylamino, or p-methoxy- benzyloxycarbonylamino; and R is a carboxy-substituted butenyl represented by the formula
have antibacterial activity.
式 1 的 4-氟氮杂环丁酮
其中 R 是羧基取代的丁烯基或酯化的羧基取代的丁烯基,其代表式为
和 R1 为氨基、氨基、亚氨基或咪唑烷基或其药学上可接受的盐从青霉素中获得,是制备 β-内酰胺类抗生素的有用中间体。式 1 的 4-氟唑烷酮类化合物,其中 R1 如上所述,但不包括氨基、苄氧羰基氨基、对硝基苄氧羰基氨基、叔丁氧羰基氨基、2,2,2-苄氧羰基氨基或对甲氧基苄氧羰基氨基;R 是羧基取代的丁烯基,其代表式为
具有抗菌活性。