NEW MATERIAL:A compound expressed by formula I [R1 is H, lower alkyl or aralkyl; R2 is (substituted) alkyl or heterocyclic ring; R3 is H or carboxyl- protecting group].
EXAMPLE: p-Nitrobenzyl (1R, 5S, 6S)-2-oxo-6-[(1R)-1-hydroxyethyl]-1- methoxycarbapenem-3-carboxylate.
USE: An antimicrobial agent and β-lactamase inhibitor.
PREPARATION: A (1R)-1-substituted-2-oxo-carbapenem-3-carboxylic acid compound expressed by formula II (R3 is carboxyl-protecting group) is reacted with an acylating agent expressed by the formula RaX (Ra is eliminative group, preferably acyl; X is halogen) or a reactive derivative thereof to give a compound expressed by formula III, which is then reacted with a mercapto reagent expressed by the formula R2SH in the presence of a base and, as necessary, the deprotection is carried out.
KUMAGAI TOSHIO
SHIMIZU HISASHI
| JPS60233077A | 1985-11-19 | |||
| JPS61275267A | 1986-12-05 |
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