反应详情

温度

35 °C

Vemurafenib (500 mg, 1.0 mmol) was suspended in 5 mL acetone at 35°. A solution of choline hydroxide in methanol (45%, 270 mg, 1.0 mmol) was added and the resulting mixture was stirred at 35° C. for 5 minutes. Then, the resulting clear solution was cooled to 5° C. over 30 minutes and was stirred in the opened vial overnight at room temperature. An oily residue was obtained and 2 mL ethanol was added. The mixture was sonicated (treated with ultra-sonic energy) until a clear solution was obtained. Two drops of n-hexane were added and the mixture was cooled in a refrigerator for 9 days. The obtained precipitate was filtered, washed with ethanol and dried under normal pressure at room temperature to yield 200 mg (33%) Vemurafenib choline as a white solid. (Purity: 98.4% by HPLC)

1. temperatureThen, the resulting clear solution was cooled to 5° C. over 30 minutes
2. stirringwas stirred in the opened vial overnight at room temperature
3. customAn oily residue was obtained
4. customThe mixture was sonicated
5. addition(treated with ultra-sonic energy) until a clear solution
6. customwas obtained
7. temperaturethe mixture was cooled in a refrigerator for 9 days
8. filtrationThe obtained precipitate was filtered
9. washwashed with ethanol
10. customdried under normal pressure at room temperature