【摘要】 按照药物拼合原理,在黄酮分子中引入具有降血脂作用的丹皮酚(5,中药丹皮的有效成分)和非诺贝特的结构特征:对羟基苯甲醛(2)与氯乙酸乙酯通过Williamson反应制得对醛基苯氧基乙酸乙酯(3);3水解得对醛基苯氧基乙酸(4);4与5经羟醛缩合制得(E)-2-{4-[3-(2-羟基-4-甲氧基苯基)-3-氧代丙烯-1-基]苯氧基}乙酸(6);I2催化6完成分子内环合制得新型黄酮类衍生物——2-[4-(7-甲氧基-4-氧-4H-吡喃-2-基)苯氧基]乙酸,总收率21.8%,其结构经1HNMR,13C NMR,IR和MS表征。更多还原

【Abstract】 The structure characteristics of Paeonol(5,a useful compounds of chinese traditonal medicine) and Fenofibrate were introduced in flavone molecular on the drug piece together principle to obtain a novel flavone derivative.(p-Formylphenoxy)acetic acid(4) was prepared by Williamson reaction of p-hydroxylbenzaldehyde with ethyl chloroacetate,then hydrolysis.Targeted compound 2-[4-(7-methoxypheny-4-oxo-4H-pyrane-2-yl)phenoxy]acetic acid in overall yield of 21.8% was synthesized by aldol condensation reaction of 4 and 5,then intramolecular cyclization reaction catalyted by I2.The structures were characterized by 1H NMR,13C NMR,IR and MS.更多还原