摘要/Abstract

以4-羟基香豆素和邻胺基苯甲醛为原料, 高效合成了具有药物活性的3-位邻羟基苯甲酰基单取代的四氢喹啉衍生物. 在乙醇溶剂中, 反应经过克脑文格尔缩合/[1,5]-氢迁移/环化/水解/脱羧这五个串联过程进行. 另外, 还实现了底物控制的多样性合成, 在无催化剂、无溶剂、室温条件下制备了一系列二香豆素内盐.
关键词: 4-羟基香豆素, 氢迁移反应, 四氢喹啉, 二香豆素内盐
The pharmaceutically significant 3-mono-substituted tetrahydroquinoline derivatives carryingortho-hydroxy- benzoyl moiety are constructed via EtOH mediated cascade Knoevenagel condensation/[1,5]-hydride transfer/cyclization/hydrolysis/decarboxylation from 4-hydroxycoumarins ando-aminobenzaldehydes. In addition, the substrate-controlled diverse syntheses also could be achieved, and a variety of the zwitterionic biscoumarin derivatives are facilely provided under catalyst- and solvent-free conditions at room temperature.
Key words: 4-hydroxycoumarin, hydride-transfer reaction, tetrahydroquinoline, zwitterionic biscoumarin


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