1H-3,4-DIHYDRO-2,3-BENZOXAZINE DERIVATIVES AND PROCESS FOR THEIR PREPARATION

摘要

1,177,083. 1-H-3,4-Dihydro-2,3-benzoxazine. GRUPPO LEPETIT S.p.A. 10 April, 1967 [22 April, 1966], No. 17810/66. Heading C2C. Novel compounds of formula wherein R is hydrogen or a lower alkyl of C 1 -C 8 , halo-lower alkyl of C 1 -C 8 , dialkylamino-(lower alkyl of C 1 -C 8 ), aryl (lower alkyl of C 1 -C 8 ) optionally substituted by lower alkoxy of C 1-8 in the aryl ring, arylcarbamylmethyl, lower alkyl of C 1 -C 8 substituted with a heterocyclic nitrogen containing ring of 5-6 atoms, hydroxy-lower alkyl of C 1 -C 8 , acyloxy-(lower alkyl of C 1 -C 8 ), carbamyl, phenylcarbamyl or guanyl group or the acyl radical of a carboxylic acid are prepared from α.αSP1/SP-dibromo-o-xylene and N-hydroxyurethan in the presence of an alkali metal hydroxide and splitting off the carboethoxy group from the intermediate N-carboethoxy-1H-3,4-dihydro-2,3-benzoxazine by hydrolytic cleavage, and the N-unsubstituted 1H-3,4-dihydro-2,3- benzoxazine so obtained is then optionally treated with an agent capable of introducing the radical R above, when R is other than hydrogen. Pharmaceutical compositions having sedative, tranquillizing and anti-inflammatory activity comprise an above novel compound and a carrier therefor.