PROCESS FOR THE PREPARATION OF 1-CARBAPENEMS AND INTERMEDIATES VIA SILYL-SUBSTITUTED DITHIOACETALS

摘要

Disclosed is a process for the total synthesis of 1-carbapenem antibiotics (I) from L-aspartic acid via central intermediates II and III: where R is hydrogen, a pharmaceutically acceptable ester moiety or salt cation, or a readily removable blocking group; R<6>, R<7> and R<8> are, inter alia, independently selected from the group consisting of hydrogen, alkyl, alkenyl, aryl and aralkyl; R<1> min and R are hydrogen, or a readily removable protecting group; R, R and R are selected from alkyl, aryl or aralkyl.