1-Oxa-.beta.-lactam antibiotics
AssigneeEli Lilly and Company
InventorAllen S. Katner
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Abstract
Bicyclic 1-oxa-.beta.-lactam diacid antibiotics represented by the formula ##STR1## wherein R is phenyl, hydroxyphenyl, acetoxyphenyl, alkylphenyl, or halophenyl, thienyl or furyl; R.degree. is H or OCH.sub.3 ; and the pharmaceutically acceptable non-toxic salts thereof are broad spectrum antibiotics useful for controlling infections in man and animals. The compounds are prepared by reacting the corresponding 3-halomethyl diester with 1-cyanomethyl-1H-tetrazole -5-thiol followed by deesterification.
Claims10
A compound of the formula ##STR19## wherein R is an .alpha.-carboxysubstituted arylmethyl group of the formula ##STR20## wherein R' is hydrogen, hydroxy, protected hydroxy, acetoxy, C.sub.1 -C.sub.3 alkyl, or halogen;
- ##STR21## R.degree. is hydrogen or methoxy;
- R.sub.1 and R.sub.1 ' are hydrogen or a carboxy protecting group;
- and when R.sub.1 and R.sub.1 ' are hydrogen, the pharmaceutically acceptable non-toxic salts thereof.
The compound of claim 3 wherein R' is hydrogen, hydroxy, or acetoxy.
Dependencies are inferred from the claim text.