Lilly Industries, Inc.

Eli Lilly Industries Limited

David William Dunwell

Delme Evans

Terence Alan Hicks

Benzoxazoles substituted in the 2-position with sulfhydryl or halogen and substituted in the 5- or 6-position with an acetic or propionic acid group or a salt or ester thereof or a nitrile convertible thereto useful as intermediates in the preparation of 5- or 6-Substituted benzoxazole propionic or acetic acid derivatives, substituted in the 2-position of the oxazole nucleus by a group of the formula AR.sup.4 wherein A is --CH.sub.2 --, --CO--, --CHOR--, or --NR--, wherein R is hydrogen, C.sub.1-6 alkyl or C.sub.2-7 acyl, and R.sup.4 is optionally substituted phenyl, useful as non-steroidal, non-narcotic, analgesic, antipyretic and anti-inflammatory agents.

2,5 OR 2,6-Disubstituted benzoxazoles

5- or 6-Substituted benzoxazole propionic or acetic acid derivatives, substituted in the 2-position of the oxazole nucleus by a group of the formula AR.sup.4 wherein A is --CH.sub.2 --, --CO--, --CHOR--, or --NR--, wherein R is hydrogen, C.sub.1.sub.-6 alkyl or C.sub.2.sub.-7 acyl, and R.sup.4 is optionally substituted phenyl, useful as non-steroidal, non-narcotic, analgesic, antipyretic and anti-inflammatory agents.

2,5 OR 2,6 Disubstituted benzoxazoles

2-(Optionally substituted)phenyl-benzoxazoles having a carboxy alkyl, a tetrazolyl, or oxazolinyl group at the 5 or 6 position useful as aspirin-like non-steroidal, non-narcotic, analgesic, antipyretic and anti-inflammatory agents.

2-(Optionally substituted)phenyl-5 or 6-substituted benzoxazoles

The invention provides novel 5- and 6-benzoxazolyl alkanoic acids, optionally substituted in the 2-position, and derivatives thereof which possess anti-inflammatory, anti-pyretic and analgesic activity. Also provided is a process for preparing such compounds by cyclizing an appropriately substituted o-aminophenol and, if necessary, converting the resultant benzoxazole to the desired compound.

Cyanomethyl substituted benzoxazoles

The invention provides novel 5- and 6-benzoxazolyl alkanoic acids, optionally substituted in the 2-position, and derivatives thereof which possess anti-inflammatory, anti-pyretic and analgesic activity. Also provided is a process for preparing such compounds by cyclising an appropriately substituted o-aminophenol and, if necessary, converting the resultant benzoxazole to the desired compound.

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Camberley, United Kingdom

David William Dunwell