Process for the preparation of 1-carbapenems and intermediates via trithioorthoacetates.

摘要

Disclosed is a process for the total synthesis of 1-carbapenem antibiotics (I) from L-aspartic acid via intermediates II and III:
wherein R is hydrogen, a pharmaceutically acceptable ester moiety or salt cation, or a readily removable blocking group; R⁶ and R⁷ are, inter alia, independently selected from the group consisting of hydrogen, alkyl, alkenyl, aryl and aralkyl; R^1' is hydrogen or a protecting group; and R^a, R^b and R^C are independently selected from alkyl, aryl and aralkyl.