Process for preparing penem derivatives

Chemistry of carbon compounds – Miscellaneous organic carbon compounds – C-metal

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2602452T, C07D49900, A61K 31425

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active

045171246

ABSTRACT:
The present invention provides a process for the preparation of a compound of the formula (IV): ##STR1## or salt or ester thereof wherein R.sup.1 and R.sup.2 are independently hydrogen; an organic radical bonded via a carbon atom to the ring carbon atom; a free, etherified or esterified hydroxy or mercapto group; an amino or acylamino group; or together R.sup.1 and R.sup.2 represent a group .dbd.CR.sup.5 R.sup.6 wherein R.sup.5 and R.sup.6 are the same or different and each represent hydrogen or a hydrocarbon or heterocyclic group optionally substituted with a functional group; and R.sup.3 represents an organic radical; which process comprises reacting a compound of the formula (V): ##STR2## wherein R.sup.x is hydrogen or a blocking group and R.sup.4 is an organic radical; with a thiol or reactive derivative thereof. The compounds of the formula (IV) are useful as antibiotics and .beta.-lactamase inhibitors, as are the compounds of the formula (V). This invention also provides the novel compounds of the formula (V) and certain novel compounds within formula (IV). Their preparation and use are described.

REFERENCES:
patent: 4347183 (1982-08-01), Afonso et al.
patent: 4372965 (1983-02-01), Christensen et al.
patent: 4474793 (1984-10-01), Ross et al.

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