首页|盐酸决奈达隆的合成工艺研究

盐酸决奈达隆的合成工艺研究

扫码查看
目的 优化盐酸决奈达隆的合成工艺.方法 以5-硝基水杨醛为起始原料,经醚化、水解、环合、傅克酰化、脱甲基反应得到关键中间体2-丁基-3-(4-羟基苯甲酰基)-5-硝基苯并呋喃,再经醚化、还原、甲磺酰化和成盐反应得到目标化合物盐酸决奈达隆.结果 与结论 目标化合物及关键中间体的结构均经1H-NMR谱确证,目标化合物总收率为44.7%,纯度为99.9%,产品质量符合《欧洲药典》标准.优化后的工艺简化了实验操作,产品质量易于控制,更有利于实现工业化生产.
Study on the synthetic process of dronedarone hydrochloride
Dronedarone hydrochloride is an approved drug for the treatment of arrhythmia.A new route to dronedarone hydrochloride was optimized on the base of references and laboratory verification.Using 5-nitrosalicylaldehyde as the starting material,the target compound was afforded by etherification,hydrolysis,cyclization,Friedel-Crafts acylation,demethylation,etherification,reduction,methane sulfonylation and salt formation,with a total yield of 44.7%and purity of 99.9%(HPLC).The improved synthetic process has the advantages of simple operation,mild reaction conditions,lower technology costs,high yield and purity,which is more suitable for industrial production.

dronedarone hydrochloridesynthesisprocess optimization

石创业、张瑞文、崔宝刚、潘莉、程卯生

展开 >

沈阳药科大学 制药工程学院,辽宁沈阳 110016

大道隆达(北京)医药科技发展有限公司,北京 101102

盐酸决奈达隆 合成 工艺优化

2024

中国药物化学杂志
沈阳药科大学,中国药学会

中国药物化学杂志

CSTPCD
影响因子:0.463
ISSN:1005-0108
年,卷(期):2024.34(1)
  • 9