Cyclization process for .beta.-lactams

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United States of America Patent

PATENT NO 4675399
SERIAL NO

06783705

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Abstract

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Process for N-acyloxy or sulfooxy 2-azetidinones comprising O-acylation of a .beta.-hydroxy or .beta.-halo hydroxamic acid, and cyclizing the O-acylhydroxamate with TPP-CCl.sub.4 -TEA or with TPP-dialkylazodicarboxylate to the N-acyloxy-2-azetidinone. Solvolysis of the acyl group provides an N-hydroxy-2-azetidinone. e.g., N-Cbz-L-serine is converted to the O-acetyl hydroxamate, cyclized and solvolyzed to N-hydroxy-3-(Cbz-amino)-2-azetidinone. The N-hydroxy-2-azetidinones are useful intermediates to monocyclic .beta.-lactam antibiotics and .beta.-lactamase inhibitors.

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Patent Owner(s)

Patent OwnerAddress
NOTRE DAME UNIVERSITYNOTRE DAME IN

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Miller, Marvin J South Bend, IN 51 220

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