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盐酸维拉佐酮的合成工艺研究
引用本文:王志龙,康江鹏,潘毅,陈蔚,王立敏.盐酸维拉佐酮的合成工艺研究[J].现代药物与临床,2015,30(7):753-756.
作者姓名:王志龙  康江鹏  潘毅  陈蔚  王立敏
作者单位:1. 天津工业大学材料科学与工程学院,天津,300387
2. 天津药物研究院化学制药部,天津,300193
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。

关 键 词:盐酸维拉佐酮  5-氰基吲哚  合成
收稿时间:2015/4/16 0:00:00

Synthesis of vilazodone hydrochloride
WANG Zhi-long,KANG Jiang-peng,PAN Yi,CHEN Wei and WANG Li-min.Synthesis of vilazodone hydrochloride[J].Drugs & Clinic,2015,30(7):753-756.
Authors:WANG Zhi-long  KANG Jiang-peng  PAN Yi  CHEN Wei and WANG Li-min
Institution:School of Material Science and Engineering, Tianjin Polytechnic University, Tianjin 300387, China;Centre for Chemical Pharmaceutical Research, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China;Centre for Chemical Pharmaceutical Research, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China;Centre for Chemical Pharmaceutical Research, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China;School of Material Science and Engineering, Tianjin Polytechnic University, Tianjin 300387, China
Abstract: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.
Keywords:vilazodone hydrochloride  5-cyanoindole  synthesis
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