NEUE OXAZOLE

1412377 Oxazoloazepine derivatives DR KARL THOMAE GmbH 9 Feb 1973 [10 Feb 1972] 6476/73 Heading C2C [Also in Division A5] Novel compounds of Formula I: (wherein R represents a hydrogen atom, an alkyl group containing from 1 to 4 carbon atoms substituted by a hydroxy, carboxy or carbalkoxy group; a saturated or unsaturated aliphatic acyl group containing from 1 to 6 carbon atoms optionally substituted by a hydroxyl group; a benzoyl group optionally substituted by one or more methyl or methoxy groups or by one or more halogen atoms; or a pyridinecarbonyl or phenylacyl group) and acid addition salts thereof, are prepared by reacting a compound of Formula II with urea. Intermediates of Formula II are prepared by various methods for example by the following sequence : (i) for R = H, a compound of formula is cyclized and then the N-benzyl compound is debenzylated; (ii) for R = acetyl, the compound R = H is acetylated; (iii) for R = hydroxyalkyl, the ethylene glycol ketal of the compound R = H is reacted with ethylene oxide.