| 摘要 |
<p>The invention comprises compounds of formula <FORM:1045903/C2/1> in which R represents a straight or branched chain C1- 5 alkylene group, R1 represents a hydrogen atom or a C1- 3 alkyl, C1- 3 hydroxyalkyl, acylated C1- 3 hydroxyalkyl or C1- 5 alkoxyalkyl group, R2 and R3 which are the same or different represent hydrogen atoms or C1- 3 alkyl groups or, when taken together as an ethylene group, and in which the benzene nuclei may be substituted by one or more of halogen atoms and trifluoromethyl, C1- 3 alkyl, C1- 3 alkoxy or C1- 3 alkyltio groups; and physiologically acceptable acid-addition salts thereof. The compounds may be prepared by (a) reacting a reaction mixture containing nitrilium or imonium cations of the formulae <FORM:1045903/C2/2> with an amine of the formula <FORM:1045903/C2/3> or (b) by dehydrating a compound of the formula <FORM:1045903/C2/4> or (c) by intramolecular condensation of a compound of the formula <FORM:1045903/C2/5> in which Y represents an oxygen or sulphur atom, or (d) by reacting a primary amine of the formula <FORM:1045903/C2/6> or the amino group alkyl derivatives thereof, with reactive esters of alcohols having the formula <FORM:1045903/C2/7> or <FORM:1045903/C2/8> In each of the above Formulae II, IV, V and VI the benzene nuclei are unsubstituted or substituted as indicated for the compounds of Formula I. 2,11 - Dichloro - dibenz[b,f][1,4] - oxazepine is prepared by reacting 2-chloro-10,11-dihydro-11 - oxo - dibenz[b,f][1,4]-oxazepine with phosphorus oxychloride. Pharmaceutical compositions having neuroplegic, neuroleptic and analgesic activity, for enteral or parenteral administration, comprise a compound of the invention together with a pharmaceutically acceptable carrier.</p> |
