Ethanol → Atazanavir Sulfate

Participants

Reaction Steps

To a 20 mL sample viral equipped with a magnetic stir was charged atazanavir base (1.0 g), 99.5% EtOH (mL, 1 vol), and MeCN (4 mL, 4 vol) at 20-30° C. Concentrated sulfuric acid (0.085 mL, 1.1 equiv) was added at 20-30° C., and the resulting clear amber solution was stirred at 20-30° C. for 4 hr. The product was filtered, washed with a mixture of EtOH/MeCN (1:4, 5 mL, 5 vol), and dried under vacuum at 40-50° C. for 16 hr to afford atazanavir sulfate in Form A (0.47 g, 42% yield, 99.9% HPLC purity).

Provenance & Evidence