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目的改进抗偏头痛药夫罗曲坦的合成方法。方法以1,4-环己二酮为原料,经过羰基保护、还原胺化、Fischer indole-carbazole合成、手性拆分、成盐5步反应得到目标化合物琥珀酸夫罗曲坦。结果与结论目标化合物的结构经过1H-NMR和MS谱确证,HPLC峰面积归一化法测定纯度为99.8%,ee值为99.0%,总收率为9.7%。该路线反应条件温和,操作简便,原料易得,有利于工业化生产。
Objective To improve the synthetic method of anti-migraine drug flocilatein. Methods 1,4-Cyclohexanedione was used as the starting material to afford the target compound futritretin succinate after carbonyl protection, reductive amination, Fischer indole-carbazole synthesis and chiral resolution. Results and Conclusions The structure of the target compound was confirmed by 1H-NMR and MS. The purity was 99.8% and the ee was 99.0%. The total yield was 9.7%. The route reaction conditions are mild, easy to operate, easy to get raw materials, is conducive to industrial production.