| 摘要 |
1,135,947. Phenanthridone derivatives. ASPRO - NICHOLAS Ltd. 19 April, 1966 [20 April, 1965], No. 16662/65. Heading C2C. Novel compounds of Formula I wherein R, R 1 and R 2 each represent a hydrogen atom or a methyl radical, R 3 and R 4 represent hydrogen, or a lower alkyl, cycloalkyl or aralkyl radical, or together with the adjacent nitrogen atom form a heterocyclic ring optionally containing a further hetero atom, which hetero atom, when nitrogen, may be substituted by a lower alkyl or hydroxyalkyl group, and R 5 and R 6 represent a hydrogen or halogen atom, or a lower alkyl, alkoxy, alkylthio, trifluoromethyl, nitro, amino, hydroxyl, cyano or sulphamoyl radical, and acid addition salts thereof are prepared by reacting a phenanthridone of the formula wherein R 5 and R 6 have the above significance and Z is H or -CH(R)-CH(R 1 )-CH(R 2 )Cl, wherein R, R 1 and R 2 have the above significance, with (a) when Z is H, a compound of the formula in which Y is Cl, Br or I or an alkyl- or arylsulphonyloxy radical, in the presence of a condensing agent and (b) when Z is with an amine of the formula R 3 R 4 NH and thereafter, where a novel compound of the first formula above in which R 3 and/or R 4 is a hydrogen atom is required and is not obtained by the foregoing method, reducing the corresponding compound in which R 3 and/or R 4 is an arylmethyl radical. Therapeutic compositions having anti-depressant activity which may be administered orally, rectally or parenterally contain as active ingredient at least one compound of Formula I above or a pharmaceutically acceptable acid addition salt thereof. |
