盐酸维拉佐酮的合成工艺研究

Synthesis of vilazodone hydrochloride

目的对盐酸维拉佐酮的合成工艺进行研究。方法以5-氰基吲哚为起始原料,通过傅克反应、还原反应、磺酰化反应、缩合反应得到维拉佐酮,然后与盐酸反应得到盐酸维拉佐酮。结果合成了目标化合物,并利用1H-NMR、MS确证了结构。此路线的总收率为47.89%,质量分数为99.66%。结论该合成工艺设计合理,操作简单,适用于工业化生产,盐酸维拉佐酮的收率和纯度较高。

Objective To study the synthetic technology of vilazodone hydrochloride. Methods 5-Cyanoindole was used as starting material to synthesize vilazodone by Friedel-Craft reaction, reduction reaction, sulfonylation reaction, and condensation reaction. Then vilazodone hydrochloride was synthesized by reacting with hydrochloric acid. Results The target compound was synthesized and characterized by 1H-NMR and MS. The total yield of vilazodone hydrochloride with the purity of 99.66% was 47.89%. Conclusion The synthetic route of vilazodone hydrochloride has the advantages of reasonable design and simple operation with high yield and purity, and is suitable for industrial production.