摘要/Abstract
喹啉-2,4-二酮结构单元广泛存在于天然产物以及具有生物活性的合成化合物中.报道一种通过α,α-二烃基氰基乙酰芳胺化合物在三氟甲烷磺酸甲酯作用下的分子内Houben-Hoesch反应合成喹啉-2,4-二酮类化合物的方法.该方法具有适用范围广、操作简便、反应条件温和等优点.
关键词: 喹啉酮, 腈, 甲基化, 环化
Quinoline-2, 4-dione unit is present in many natural products and synthetic compounds along with a broad range of bioactivities. Herein, a new approach to the synthesis of quinoline-2, 4-diones is developed based on a methyl triflate (TfOMe)-promoted intramolecular Houben-Hoesch reaction of α, α-dialkyl substituted cyanoacetanilides. The broad substrate scope, simple operation and mild reaction conditions make this synthetic method very attractive.
Key words: quinolinone, nitrile, methylation, cyclization
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