Abstract
The synthesis of the four stereoisomers of 3-ethyl-4-[(4-carboxyphenyl)oxy]-1-[[(phenylmethyl)amino]carbonyl]-2-azetidinone ( 1) starting from either D or L-aspartic acid is reported. The trans (3R,4R) isomer 7a, prepared from L-aspartic acid had the most inhibitory activity against human leukocyte elastase (HLE). This monocyclic β-lactam was very resistant to hydrolysis and was found to be orally bioavailable in marmosets.
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