Water → Rosuvastatin

Participants

Reaction Conditions

Reaction Steps

Method “A”: An autoclave having 50 cm3 volume is charged with 0.89 g (1.75 mmol) of rosuvastatin N,N-dimethylamide, 35.6 cm3 of water and 2.56 g (3.7 cm3; 3.5 mmol) tert-butylamine. The reaction mixture is stirred at 120° C. for 16 hours. The mixture is allowed to cool to room temperature, the reaction mixture is diluted with ethanol in portions and evaporated in vacuo. The evaporation residue is stirred in a mixture of tert-butylmethylether and heptane (2:5 v/v, 4 cm3) and the crystals are filtered. Thus 0.87 g (90%) of rosuvastatin TBA salt are obtained. The crude salt is recrystallized from acetonitrile/2-propanol. Yield, 0.58 g (60%) rosuvastatin TBA salt having purity (by HPLC) exceeding 99.5%.

Provenance & Evidence