| 摘要 |
The invention comprises compounds of formula <FORM:1088224/C2/1> wherein X represents a nitro or amino group and Y represents a hydrogen atom or alkyl group having up to six carbon atoms, and acid addition salts thereof, and the preparation thereof by reacting a nitrobenzamidoacetonitrile under anhydrous conditions with an alcohol ROH (where R represents an alkyl group containing up to 6 carbon atoms) in an inert organic solvent, saturating the reaction mixture with anhydrous hydrogen chloride, separating the resultant imino-ether hydrochloride and reacting it in an anhydrous alcohol ROH with ammonia at a temperature below 20 DEG C., and optionally reducing the nitro group in the nitrobenzamidoacetamidine hydrochloride product to a primary amino group, and, if desired, converting the hydrochloride product into the free base. The nitrobenzamidoacetonitrile starting materials may be prepared by reacting an aminoacetonitrile with a nitrobenzoic acid halide. Therapeutic compositions, which may be administered orally, rectally or parenterally, comprise as active ingredient at least one compound of Formula (I) above, or a non-toxic acid-addition salt thereof. Compounds in which X represents an amino group show an especially marked anti-depressive action. |
