STUDIES ON THE SYNTHETIC METHODS OF 4-UNSUBSTITUTED MONOCYCLIC BETA-LACTAM ANTIBIOTICS
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Abstract
The key intermediate of monocyclic beta-lactams, N-benzyloxycarbonyl-3 S-amino-2-oxoazetidine(Ⅲ),was synthesized from L-( + )-2,3-diaminopropanoie acid(Ⅰ) by Ph3P—(PyS)2—CH3CN system and N-benzyloxycarbonylation. Ⅰ was prepared from L(+)-aspartic acid by Schmidt rearrangement.Three derivatives(Ⅷa~c) of this monocyclic beta-lactam were prepared and their biological activities evaluated.
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