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研究了在微波促进下N-对甲苯基乙酰胺与取代苯乙酸经酰化和环化反应合成2,6-二甲基-3-芳基-4(1H)-喹啉酮化合物的方法,反应时间短,产物收率高,操作简便。在微波辐射下,以BF3·Et2O为催化剂,N-对甲苯基乙酰胺与取代苯乙酸发生酰化,80℃下反应15 min,以85.7%~91.3%的收率得到中间产物N-[4-甲基-2-(2-芳基乙酰基)苯基]乙酰胺;中间产物在叔丁醇钠/叔丁醇存在下进行环化,微波辐射下回流反应20 min,得到目标产物2,6-二甲基-3-芳基-4(1H)-喹啉酮,收率89.2%~94.3%。用IR、1HNMR和元素分析确证了目标产物的结构。
A method for the synthesis of 2,6-dimethyl-3-aryl-4 (1H) -quinolinone compounds by acylation and cyclization of N-p-tolyl acetamide and substituted phenylacetic acid under microwave irradiation was studied. Short reaction time, high product yield and easy operation. Under microwave irradiation, N-p-tolyl acetamide and substituted phenylacetic acid were acylated with BF3 · Et2O as a catalyst and reacted at 80 ℃ for 15 min. The yield of N- [4 The intermediate product was cyclized in the presence of sodium tert-butoxide / tert-butanol under microwave irradiation for 20 min to obtain the target product 2, 6-dimethyl-3-aryl-4 (1H) -quinolinone in 89.2% ~ 94.3% yield. The structure of the target product was confirmed by IR, 1HNMR and elemental analysis.