三氯化铝络合橙皮苷半合成地奥司明的方法

发布时间：2018-12-17 07:17

【摘要】：目的改进地奥司明的半合成路线。方法橙皮苷与三氯化铝络合,溶于甲醇中,以吡啶为除酸剂,碘为脱氢剂,生成地奥司明络合物,再经磷酸脱铝离子,即得到地奥司明。结果以橙皮苷计,地奥司明的收率为96.4%,纯度为93.7%,熔点为278.6℃,在254、266、345 nm处有最大吸收,与对照品在薄层色谱上的Rf值和显色情况一致。结论该合成路线中的吡啶用量减少80%,反应体系为溶液型,条件温和,后处理简单,收率较高,具有工业化生产能力。
[Abstract]:Objective to improve the semi-synthetic route of Diosmin. Methods Diosmin complex was formed by complexing hesperidin with aluminum trichloride, dissolved in methanol, pyridine as acid remover, iodine as dehydrogenant, and then dealuminized by phosphoric acid. Results based on hesperidin, the yield of Diosmin was 96.4, the purity was 93.7, the melting point was 278.6 鈩，

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