| 摘要 |
The invention comprises compounds of the general formula <FORM:1025579/C2/1> wherein R represents hydrogen or <FORM:1025579/C2/2> where R1 represents hydrogen or alkyl of one to three carbon atoms and R2 represents hydrogen or alkyl of one to four carbon atoms and acid addition and quaternary ammonium salts thereof, and the preparation thereof by reacting compounds of the formulae <FORM:1025579/C2/3> wherein R1 has the above significance with an alkyl halide in the presence of an alkaline condensing agent or by reacting 1,3,4,5-tetrahydropyrrolo[4,3,2-de] quinoline with the required alkanoic anhydride and reducing the product in which R is R1>C=O with LiAlH4 or LiBH4 when the compound having R equal to <FORM:1025579/C2/4> is required, and 1,3,4,5-tetrahydropyrrolo[4,3,2-de] quinoline is prepared by treating 4-nitro-3-indolyl acetonitrile (which is prepared by reacting 4-nitrogramine with dimethyl sulphate to produce 4-nitrogramine methosulphate and then reacting with sodium sulphide) with hydrogen in the presence of a hydrogenation catalyst in the presence of an inert solvent. Pharmaceutical compositions having sedative and anti-inflammatory activity contain as the active ingredient compounds of the first formula given above. The compositions may be in the form of tablets, powder packets, capsules, solutions or suspensions suitable for oral or parenteral administration. |
