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目的:化学全合成金雀异黄素衍生物7-二氟甲氧基-5,4′-二甲氧基异黄酮。方法:以间苯三酚和对甲氧基苯乙腈为原料,经Hoesch反应、増碳环合反应得到异黄酮母核,再经二氟甲醚化、甲醚化得到目标产物。结果:目标化合物及中间体的结构均经核磁共振氢谱确证,总收率15.6%。结论:该合成路线较短,操作简单,成本较低,适合工业化生产。
OBJECTIVE: To chemically synthesize genistein derivatives 7-difluoromethoxy-5,4’-dimethoxyisoflavone. Methods: Using phloroglucinol and p-methoxyphenylacetonitrile as raw materials, the isoflavone mother nucleus was obtained by the reaction of Hoesch and carbonization and cyclization, then the target product was obtained by the difluoromethyl etherification and the methyl etherification. Results: The structures of target compounds and intermediates were confirmed by 1H NMR. The total yield was 15.6%. Conclusion: The synthesis route is short, simple operation, low cost, suitable for industrial production.