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氢氟噻嗪的合成研究

Study on synthesis of hydroflumethiazido
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摘要 本文以间三氟甲基苯胺和氯磺酸为原料,四氯乙烷为溶剂,氯磺化阶段加入Na2SO4,成功合成了5-三氟甲基-2,4-二磺酰氯苯胺中间体;所得中间体进一步与氨水反应得到5-三氟甲基-2,4-二磺酰胺苯胺;最后在弱酸性条件下与甲醛关环合成得到目标化合物3,4二氢-6-三氟甲基-2H-1,2,4-苯并噻二嗪-7-磺胺-1,1-二氧化物(氢氟噻嗪).该工艺有效地减少了废酸的产生,污染小,收率高,为此类结构的合成研究提供了实用及理论依据. The intermediate compound of 5- trifluoromethyl- 2,4- bis ( sulfonchloride ) aniline was synthesized with m- triflu- oromethyl-aniline and chlorosulfon-ic acid as raw materials. In the reaction tetrachloroethane was used as solvent, adding the sodium sulfate in chlorosulfonation stage reaction. Furthermore, the intermediate above reacted with ammonia to gain the product of 5- trifluoromethyl- 2,4 - bis (sulfonamid) aniline. Lastly, the target compound of 3,4 - dihydro- 6 - (trifluoromethyl) - 2H- 1,2,4- benzothiadiazine- 7- sulphonamide- 1,1- dioxide (hydroflumethiazide) was gained with the ring- closure reaction of formaldehyde. This process not only reduce the production of waste acid, decreased pollution, but also reach a high yield, which provide theoretical basis for the studies on the synthesis of this kind of componuds.
出处 《天津理工大学学报》 2013年第2期50-53,共4页 Journal of Tianjin University of Technology
关键词 氢氟噻嗪 5-三氟甲基-2 4-二磺酰氯苯胺 氯磺酸 合成 hdyroflumethiazide 5- trifluoromethyl- 2,4- bis (sulfonchloride) aniline chlorosulfonic acid synthesis
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