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加锡果宁(Edulinine)系河南省中医研究所常志青等从芸香科植物 Zanthoxylum simalans Hance的根及根皮中分得的取代喹啉酮生物碱,曾研究过它的肌松作用并作过临床观察。其化学结构与Iriarte等从Rulaceous树的加锡弥罗果Casimiroa Edulik中分得的相同,化学名:4-甲氧基-1-甲基-3-(2,3-二羟基-3-甲基丁基)喹啉酮-2(V)。Boyd等也曾从植物中分得化合物Ⅳ_b,经水解制得Ⅴ,并确定了该化合物的结构。鉴于该化合物具有一定生物活性,我们试探了它的合成方法,以便扩大药源作深入研究,进而改造结构探讨其构效关系。文献曾报道将3-甲基丁烯-2-基丙二酸二乙酯(Ⅰ)和N-甲基苯胺在二苯醚内进行高
Edulinine is a substituted quinolinone alkaloid derived from the root and root bark of Zanthoxylum simalans Hance, a rye plant belonging to the Henan Institute of Traditional Chinese Medicine Changzhi Qing and studied its muscle relaxant effect After clinical observation. Its chemical structure is the same as that of Iriarte et al., Obtained from Casimiroa Edulik of Rulaceous tree, and its chemical name is 4-methoxy-1-methyl-3- (2,3-dihydroxy- Butyl) quinolinone-2 (V). Boyd et al. Also isolated the compound Ⅳ_b from the plant and hydrolyzed to obtain the Ⅴ, and confirmed the structure of the compound. In view of the biological activity of this compound, we explored its synthesis method in order to expand the source of the drug for further study, and then transform the structure to explore its structure-activity relationship. It has been reported in the literature that 3-methylbutene-2-ylmalonate diethyl (I) and N-methylaniline in diphenyl ether high