| 摘要 |
1340898 Dibenzoxazepine derivatives AMERICAN CYANAMID CO 29 Sept 1971 [26 Oct 1970] 45427/71 Heading C2C Novel compounds of Formula VIII (in which X is >NH, >NCH 3 or their acid addition salts, and intermediates therefor, are prepared according to the following reaction scheme: (in which R is methyl, acetyl, benzyl, carbobenzyloxy or trifluoroacetyl). The conversion of compounds III to compounds IV and compounds VII to compounds VIII is effected by treatment with a halogenating agent to form an imino halide and reaction of this compound with the desired piperazine derivative. The nitration processes result in a mixture of 7- and 9-nitro isomers which are separated by known methods. The conversion of compounds V to compounds VII and compounds VI to compounds VIII may be effected by diazotization, reaction of the diazonium salt with acetic anhydride to form a 7-acetoxy derivative and treatment of this with a hydroxylic base. In the conversion of compounds VII to compounds VIII, the hydroxyl function may be protected, e.g. by an acetyl group. Pharmaceutical compositions comprise a compound I or acid addition salt thereof together with a pharmaceutical carrier. The compositions have CNS activity and may be administered orally or parenterally. |
