3-三氟乙酰基吲哚的合成研究

Synthesis of 3-(trifluoroacetyl) indole

以廉价易得的吲哚和三氟乙酸酐为原料,经过傅-克酰基化反应合成得到目标化合物3-三氟乙酰基吲哚,其结构经~1H-NMR和ESI-MS表征。对3-三氟乙酰基吲哚的合成工艺进行研究,确定适宜的反应条件为:物料比为n(三氟乙酸酐)∶n(吲哚)=7∶1,过量的三氟乙酸酐在反应过程中不但是反应物,而且起到溶剂的作用,反应温度为25℃,反应时间4h。在该反应条件下,产物收率为87.5%(以吲哚计)。

The target compounds 3-(trifluoroacetyl) indole was synthesized through Friedel-Crafts acylation reaction by using the readily available and cheap starting materials of indole and trifluoroacetic anhydride.The structures of product was characterized by ~1H-NMR and ESI-MS.Also, the synthesis process was studied and the suitable reaction conditions were determined as follows: material ratio n(trifluoroacetic anhydride)∶n(indole)= 7∶1,the excess of trifluoroacetic anhydride not only played the role of reactant, but also regarded as reactive solvent in the synthesis of 3-(trifluoroacetyl) indole.Reaction temperature was 25℃,reaction time 4 h.Under these conditions, the yield of the product was up to 87.5%(calculated based on indole).