申请人:BEECHAM GROUP PLC
公开号:EP0044142A1
公开(公告)日:1982-01-20
The present invention provides a process for the preparation of antibacterially active carbapenems of the formula:
and salts and esters thereof wherein R1 and R2 are independently hydrogen or an organic group bonded via a carbon atom and R3 is a group NR4R5 wherein R4 optionally substituted alkyl, aryl and aralkyl, and R5 is hydrogen or optionally substituted alkyl or R3 is optionally substituted aryl or alkyl: which process comprises the reaction of a C-3 mercapto carbapenem with an aziridine (CH2)2NCOR3.
本发明提供了一种制备具有抗菌活性的式碳青霉烯类化合物的工艺:
及其盐和酯 其中 R1 和 R2 独立地为氢或通过碳原子键合的有机基团,R3 为基团 NR4R5,其中 R4 为任选取代的烷基、芳基和芳烷基,R5 为氢或任选取代的烷基或 R3 为任选取代的芳基或烷基:该工艺包括 C-3 硫代碳青霉烯与氮丙啶 (CH2)2NCOR3 反应。