7-二氟甲氧基-5,4′-二甲氧基异黄酮的全合成

Total Synthesis of 7-Difluoromethoxy-5,4′-Dimethoxy Isoflavone

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 total synthesize Genistein's derivative 7 -difluoromethoxy -5,4′ -dimethoxy isoflavone. Methods The target compound were synthesized by phloroglucinol and p-methoxy phenylacetonitrile through Hoesch reaction and carbon-adding cyclization to get the isoflavone, then through difluoromethylation and methylation. Results The structures of the target compound and it's intermediates were confirmed by 1H-NMR , the overall yield was 15.6%.Conclusion The process was short in steps, easy to control , low in cost and practice in industrialize.