4-(5- And 7-)benzoylindolin-2-ones and pharmaceutical uses there

Details 4-(5- And 7-)benzoylindolin-2-ones and pharmaceutical uses there 4-(5- And 7-)benzoylindolin-2-ones and pharmaceutical uses there

1975-01-29

1976-08-17

Gotts, Lewis

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Fungus, except allergen, or component thereof or substance...

260325R, 26032613R, 260470, 260471R, 260516, 260518R, C07D20934, A61K 3140

Patent

active

039755312

ABSTRACT:
Novel 4-(5- and 7-)benzoylindolin-2-ones of the formula: ##SPC1##
Wherein R is hydrogen, lower-alkyl, or methylthio, R.sup.1 is hydrogen or lower-alkyl, R.sup.2 is lower-alkyl, lower-alkoxy, halogen, nitro or trifluoromethyl, R.sup.3 is hydrogen, halogen or lower-alkoxy, and n is 0, 1 or 2, are prepared by (a) acylation of indolin-2-one to give 5-benzoylindoline-2-one, (b) cyclization of 2-acetamido-3-benzoylphenylacetic acid or ethyl 2-acetamido-3-benzoylphenylacetate to give 7-benzoyindoline-2-one, or (c) by reacting aminobenzophenones with alkyl .alpha.(methylthio)acetates to give alkyl 2-amino-3-(5- or 6-)benzoyl-.alpha.-(methylthio)phenylacetates which are cyclized and demethylthiolated to 4-(5- and 7-)benzoylindolin-2-ones. The novel compounds possess anti-inflammatory activity and are intermediates for the preparation of 2-amino-3-(5- or 6-) benzoylphenylacetic acids which posess anti-inflammatory properties.

REFERENCES:
patent: 3679701 (1972-07-01), Hester

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