| 摘要 |
<p>1. Claims for the Contracting States : BE, CH, DE, FR, GB, IT, LI, LU, NL, SE 3H-2-Benzazepines of the general formula see diagramm : EP0041627,P28,F2 wherein X signifies hydrogen, chlorine or bromine, Y signifies hydrogen, fluorine or chlorine, the dotted line signifies an optional bond, n signifies the number 0 or 1, R1 signifies hydrogen, bromine, chlorine, iodine or a residue of the formula see diagramm : EP0041627,P28,F3 or see diagramm : EP0041627,P28,F4 and R2 signifies hydrogen, (C1 -C7 )-alkyl, hydroxy, amino, (C1 -C7 )-alkylamino or di-(C1 -C7 )-alkylamino and R3 signifies hydroxy or amino, with the proviso that X and Y do not both signify hydrogen, and that the dotted line signifies an additional bond when R1 does not signify hydrogen, and pharmaceutically acceptable salts thereof. 1. Claims for the Contracting State : AT A process for the manufacture of 3H-2-benzazepines of the general formula see diagramm : EP0041627,P32,F1 wherein X signifies hydrogen, chlorine or bromine, Y signifies hydrogen, fluorine or chlorine, the dotted line signifies an optional bond, n signifies the number 0 or 1, R1 signifies hydrogen, bromine, chlorine, iodine or a residue of the formula see diagramm : EP0041627,P32,F2 or see diagramm : EP0041627,P32,F3 and R2 signifies hydrogen, (C1 -C7 )-alkyl, hydroxy, amino, mono-(C1 -C7 )-alkylamino or di-(C1 -C7 )-alkylamino and R3 signifies hydroxy or amino, with the proviso that X and Y do not both signify hydrogen, and that the dotted line signifies an additional bond when R1 does not signify hydrogen, and of pharmaceutically acceptable salts thereof, characterized by a) cyclizing a compound of the general formula see diagramm : EP0041627,P32,F4 wherein X and Y have the above significance and the dotted line signifies an optional bond, or b) oxidizing a compound of the general formula see diagramm : EP0041627,P32,F5 wherein X and Y have the above significance, R11 signifies hydrogen, bromine, chlorine or iodine and the dotted line signifies an optional bond, with the proviso that the dotted line signifies an additional bond when R11 does not signify hydrogen, or c) dehydrohalogenating a compound of the general formula see diagramm : EP0041627,P33,F1 wherein X and Y have the above significance and R12 signifies chlorine, bromine or iodine, or d) reacting a compound of the general formula see diagramm : EP0041627,P33,F2 wherein X, Y, n and R12 have the above significance, with a compound of the general formula HC -= C-CH2 -R21 wherein R21 signifies hydrogen, (C1 -C7 )-alkyl, hydroxy, mono-(C1 -C7 )-alkylamino or di-(C1 -C7 )-alkylamino, in the presence of a palladium salt, copper (I) iodide, an organophosphine and a secondary or tertiary amine, or e) cleaving off the phthaloyl group(s) in a compound of the general formula see diagramm : EP0041627,P33,F3 or see diagramm : EP0041627,P33,F4 wherein X, Y and n have the above significance and Phth signifies phthalimido, and, if desired, f) converting a compound of general formula I obtained into a pharmaceutically acceptable salt.</p> |
