| 摘要 |
PURPOSE: Antibacterial carbapenem derivatives which are active against resistant strains are provided. They are pyrrolidine thiol carbapenems represented by formula(1), wherein R1 is hydrogen, substituted or unsubstituted lower alkly, heterocycles containing N or S, sulfonyl substituted with lower alkyl, carbonyl substituted with heterocycles containing N or S, benzyl, amide or hydroxy group; R2 is hydrogen, hydroxy alkyl, amide or ester group. CONSTITUTION: The method of preparation comprises: reacting phosphate compound with thiol derivatives represented by formula(2) under base and obtaining protected carbapenem derivatives; de-protecting them using hydrogen and palladium as a catalyst; and purifying with porous resin and freeze drying. In formula (2), R1 and R2 are same as in formula(1) and PNZ is p-nitrobenzyloxycarbonyl group.
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