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抗真菌药卤普罗近的合成
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Abstract:
从绿色化学的理念出发，探索了快速两步合成抗真菌药物卤普罗近的新方法：以2,4,5-三氯苯酚与溴丙炔为原料，用水作为溶剂，在碱性条件下加入四丁基碘化铵得到2,4,5-三氯苯基-γ-丙炔醚之后，经过萃取简单后处理，随即加入N-碘代琥珀酰亚胺和硝酸银在丙酮中继续反应可合成抗真菌药物卤普罗近。整个反应在较短时间(20 min)左右获得较高的总产率(88%)。该方法为抗真菌药物卤普罗近的环境友好合成提供了新策略，值得推广应用。
From the concept of green chemistry, a new rapid two-step synthesis for the antifungal drug haloprogin was explored: 2,4,5-trichlorophenyl-γ-propynyl ether was obtained by using 2,4,5-trichlorophenol and bromopropyn as raw materials and using tetrabutylammonium iodide as phase transfer catalyst (PTC) in water under alkaline conditions. After a simple extraction, N-iodosuccinimide (NIS) and silver nitrate (AgNO3) were added in acetone for further reaction to synthesize the antifungal drug haloprogin. The whole tandem reaction was carried out within a relatively short time (about 20 minutes) with high total yield (88%). This method provides a new strategy for the environmentally friendly preparation of the antifungal drug haloprogin and is worthy of promotion and application.
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