盐酸维拉佐酮的合成工艺研究
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摘要
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.
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.
引文
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[3]王启发,程青芳,陈娜,等.盐酸维拉唑酮的合成[J].中国医药工业杂志,2013,44(1):3-12.
[4]吕天翔,张灿,胡春.维拉佐酮合成路线图解[J].中国药物化学杂志,2012,22(1):74-81.
[5]默克专利股份有限公司.制备5-(4-[4-(5-氰基-3-吲哚基)-丁基]-1-哌嗪基)-苯并呋喃-2-甲酰胺的方法[P].中国:101163698B,2011-05-18.
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