盐酸决奈达隆的合成工艺改进

Improved Synthesis of Dronedarone Hydrochloride

以2-丁基-3-(4-羟基苯甲酰基)-5-硝基苯并呋喃为原料,通过醚化、催化氢化、甲磺酰胺化、N-烃化及成盐等反应合成盐酸决奈达隆,总收率为70.6%,产物经NMR和MS等谱图确证。该工艺原料易得,条件温和,产率较高,适合工业化生产。

Dronedarone hydrochloride was synthesized by a serial reactions of etherification,catalytic hydrogenation,methsulfonamidation,N-alkylation and salt-forming from 2-butyl-3-（4-hydroxybenzoyl）-5-nitrobenzo-furan. The overall yield was about 70. 6%,and the structure of the product was confirmed by NMR and MS.The process route is easy to obtain raw materials with mild conditions and high yield. Thus it is suitable for industrial production.