反应详情

温度

30 °C

Rosuvastatin tert-butyl ester (3.0 g, 5.6 mmol) is dissolved in 25 mL of a 4:1 mixture of THF/water. The clear solution is warmed to 30° C. and 8.0 M NaOH (0.75 mL, 6.0 mmol) was added portionwise. The reaction mixture is stirred at 30° C. for 2 hours giving a clear yellow solution. Then THF is removed completely under the reduced pressure (20 mbar) at 40° C. The remaining aqueous solution is diluted with water to 25 mL and washed with AcOEt (2×10 mL). After separation from the organic layer aqueous phase is distilled under the reduced pressure (20 mbar) at 40° C. to completely remove the dissolved AcOEt. The remaining clear solution of sodium rosuvastatinate is diluted with water to 25 mL and liophylized to afford 2.81 g (100%) of rosuvastatin sodium salt as white powder.

1. customgiving a clear yellow solution
2. customThen THF is removed completely under the reduced pressure (20 mbar) at 40° C
3. additionThe remaining aqueous solution is diluted with water to 25 mL
4. washwashed with AcOEt (2×10 mL)
5. customAfter separation from the organic layer aqueous phase
6. distillationis distilled under the reduced pressure (20 mbar) at 40° C.
7. customto completely remove the dissolved AcOEt
8. additionThe remaining clear solution of sodium rosuvastatinate is diluted with water to 25 mL