The preparation of a number of 1,4-benzodiazepines substituted in the 3 position is described. The rearrangement of 7-chloro-l,3-dihydro-5-phenyl-2H-l,4-benzodiazepin-2-one 4-oxide with diacetyl sulfide yields largely the 3-acetylthio compound. Amines, ethers, and sulfides were prepared through the chloro intermediate. A 3-carbethoxybenzodiazepine was prepared and converted into oxazepam. The pharmacological test data of new and previously published compounds are given.
The uxazole, oxaprozin has a spectrum of activity in various in vivo and in vitro, chronic and acute inflammatory models in 3 species indicating that it belongs to the general class of non-steruidal anti-inflammatory agents. Possible advantageous features of oxaprozin over existing nonsteroidal anti-inflammatory agents include relative safety, minimal irritant properties on the gastrointestinal tract, long half-life, and urieosurie properties.
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