| 摘要 |
1,138,753. 1,2,8,9 - Tetraazaphenalene and derivatives thereof. J. R. GEIGY A.G. 4 April, 1966 [4 April, 1965], No. 14762/66. Heading C2C. Novel compounds having the formula and their addition salts and quaternary ammonium compounds, wherein R 1 is H or C 1-6 alkyl and R 2 is H, Hal., OH, COOH or C 1-6 alkoxy, may be prepared, either by heating a compound of formula wherein R 2 is as defined above, and A is -CHO or a group whose oxidative state corresponds to that of the CHO group and which can be bound to the COOH group to form a lactone, with at least two equimolecular amounts of hydrazine hydrate; or by heating a compound of formula wherein R 1 , R 2 and A are as previously defined, with at least one equimolecular amount of hydrazine hydrate, and in each case isolating the product and, if desired, converting it to an addition salt with an organic or inorganic acid, or transforming it to a quaternary ammonium compound with a C 1-6 alkylating agent. 4 - Substituted - 2,6 - bis - (dibromomethyl) - benzoic acids are made by bromination of the corresponding 2,6 - dimethyl - benzoic acids. Methyl - 4 - carboxy - 2,6 - bis - (dibromomethyl) - benzoate is also prepared analogously. 5 - Substituted - 3 - hydroxy - 7 - aldehydophthalides are prepared by hydrolysis of corresponding 4 - substituted - 2,6 - bis - (dibromomethyl)-benzoic acids. These compounds are tautomeric, thus: 8 - Aldehydo - 1(2H) - phthalazinone hydrazone is prepared by the reaction of hydrazine hydrate on 3-hydroxy-7-aldehydophthalide. Pharmaceutical compositions comprise at least one compound of the first formula given above, or a pharmaceutically acceptable salt or quaternary ammonium compound thereof, together with at least one pharmaceutically acceptable carrier. They have sedative, hypotensive and cardiovascular activity and may take the forms of tablets, capsules, powders, suspensions, solutions or syrups, and may be administered orally or parenterally. |
