反应详情

温度

5 °C

Under a temperature range from room temperature to reflux temperature, preferably reflux temperature, 5-amino-2-butyl-3-(4-[3-(dibutylamino)propoxy]benzoyl)benzofuran is reacted with methanesulfonyl chloride in acetonitrile solvent to provide a crude dronedarone hydrochloride, wherein an amount of acetonitrile used is in the range of 0 to 10 parts by volume, preferably 1 to 8 parts by volume, more preferably 3 to 6 parts by volume based on 1 part by weight of the compound A, and an amount of methanesulfonyl chloride used is in the range of 1 to 5 equivalents, and preferably 1.1 to 3 equivalents, and more preferably 1.2 to 2.5 equivalents relative to the compound A to obtain a reaction mixture. When the reaction is terminated, the reaction mixture is cooled to −30 to 50° C., preferably −20 to 35° C., more preferably −15 to 25° C. to obtain crude dronedarone hydrochloride. Then the crude dronedarone hydrochloride can be purified to obtain highly pure dronedarone hydrochloride. If desired, the obtained dronedarone hydrochloride can be converted to highly pure dronedarone via alkaline solvent, or further converted to other pharmaceutically acceptable salts of dronedarone.

1. customto obtain a reaction mixture
2. customWhen the reaction is terminated
3. customto obtain crude dronedarone hydrochloride
4. customThen the crude dronedarone hydrochloride can be purified