| 摘要 |
<p>1,170,778. Benzazonine and benzazecine derivatives. SANDOZ Ltd. 2 Dec., 1966 [6 Dec., 1965; 7 Dec., 1965], No. 54154/66. Heading C2C. Novel compounds of the general Formula (I) in which R 1 and R 2 independently signify H or a C 1 -C 4 alkoxy radical, R 3 is H, phenyl or benzyl, R 4 is C 1 -C 4 alkyl and n is 1 or 2 and their acid addition salts are prepared by reacting a compound of general Formula (II) wherein Hal is Cl, Br or I and R 1 , R 2 , R 3 , R 4 and n are as above defined with an alkali metal in liquid ammonia and optionally converting to the salt form. The intermediates of general Formula (II) are prepared by treating a compound of general Formula (III) with a C 1 -C 4 alkyl chloride, bromide or iodide in a cyclic or open chain ether, alone or in the presence of another inert solvent. The starting materials of general Formula (III) are prepared by treating a compound of general formula with a chloroformic acid alkyl ester in the presence of an acid binding agent to yield a compound of general formula wherein alk is lower alkyl; which is then treated with a suitable phenylethylamine to give a compound of general formula This compound is then cyolized to yield the keto compound of formula which is treated with lithium aluminium hydride in a cyclic or open chain ether to reduce the keto group and yield the required product. The starting material 8,9-dimethoxy- 105 - benzyl - 1,2,3,5,6,10b - hexahydro - pyrrolo- [2,1a] - isoquinoline is prepared by refluxing 8,9 - dimethoxy - 2,3,5,6 - tetrahydro - 1H- pyrrolo - [2, la] - isoquinilium bromide with a benzyl Grignard reagent. The bimaleate of this starting material is also prepared. Pharmaceutical compositions possessing antidepressive and when n is 1, bradycardiac properties, comprise compounds of the Formula (I) or the pharmaceutically acceptable acid addition salts thereof and a carrier. Reference has been directed by the Comptroller to Specification 993,156.</p> |
