| 摘要 |
1468913 Sulphamoylbenzoic acid derivatives CIBA-GEIGY AG 1 July 1974 [10 July 1973] 29097/74 Heading C2C Novel compounds of formula where R 1 is C 1-7 alkyl, R 2 is H, halogen, CF 3 , C 1-7 alkyl or C 1-7 alkoxy, R 3 is H, OH or C 1-7 alkyl, R 4 is -A-Y-R 5 , where A is C 1-7 alkyl or alkenyl, Y is a hetero atom or a direct bond and R 5 is aryl, and alk denotes C 1-7 alkylene separating the N atoms by 2 or 3 C, are prepared by: (a) reducing the nitro group in (b) reacting where R<SP>1</SP> 3 is H or C 1-7 alkyl with or (c) splitting of X from where X is acyl (broadly used); and if desired introducing, modifying or splitting off substituents as appropriate. 1 - [5 - Dimethylsulphamoyl)- N - acetylanthraniloyl] - 4 - benzylpiperazine is prepared by acetylating the corresponding anthraniloyl compound and is then subjected to hydrogenative debenzylation to give 1-[5-dimethylsulphamoyl) - N - acetylanthraniloyl] - piperazine which is reacted with hydratropaldehyde and HCOOH to give 1-[5-dimethylsulphamoyl-2-acetamidobenzoyl] - 4 - (2 - phenylpropyl) - piperazine. 5 - (Dimethylsulphomoyl) - 2 - nitrobenzoylchloride is obtained by the action of thionyl chloride on the acid and is then converted to the N-phenylethylpiperazide. The compounds of the first formula above as antiinflammatory and analgesic agents.
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