Spirocyclic 6-amido-carbapenems and azetidinones
AssigneeMerck & Co., Inc.
InventorsMark L. Greenlee, Thomas N. Salzmann, Frank P. DiNinno
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Abstract
New antibacterial spirocyclic 6-amido carbapenems of the structural formulas: ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-8 substituted or unsubstituted alkyl, or C.sub.6-10 substituted or unsubstituted aryl; R.sup.5 is hydrogen or a protecting group for alcohol; R.sup.6 is hydrogen or a protecting group for amido nitrogen; R.sup.7 is hydrogen or a protecting group for amido nitrogen; and R.sup.8 is hydroxy, hydrogen, C.sub.1-8 substituted or unsubstituted thioalkyl, C.sub.6-10 substituted or unsubstituted thioaryl, 5 or 6 membered, substituted or unsubstituted thioheteroaryl; and a process for their synthesis through novel spirocyclic 4-amido azetidinones are disclosed.
Claims11
A compound of the structural formula:
- wherein R.sup.1 is hydrogen, C.sub.1-8 alkyl or C.sub.6-10 aryl;
- R.sup.7 is hydrogen or a protecting group for amido nitrogen;
- and R.sup.8 is hydroxy, hydrogen, C.sub.1-8 alkylthio cyano-C.sub.2 alkylthio, C.sub.6-10 arylthio, or 2-pyridylthio.
A compound of the structural formula:
- ##STR44## where R.sup.5 is hydrogen or a protecting group for alcohol;
- R.sup.6 is hydrogen or a protecting group for amido nitrogen;
- R.sup.7 is hydrogen or a protecting group for amido nitrogen;
- and R.sup.1 is hydrogen, C.sub.1-8 alkyl, or C.sub.6-10 aryl;
- with the condition that R.sup.6 and R.sup.7 as protecting groups are separately cleavable.
Dependencies are inferred from the claim text.