Ethanol → Atazanavir Sulfate

Participants

Reaction Conditions

Reaction Steps

0.085 mL of sulfuric acid (concentrate, 1.1 equiv) was added into the mixture of 1 g of atazanavir base, 7.5 mL of EtOH (7.5 vol) and 7.5 mL of MTBE (7.5 vol) at 20-30° C. The resulting clear amber solution was stirred at 20-30° C. for 4 hr. The product was filtered, washed with a mixture of EtOH/MTBE (1:2, 3 mL, 3 vol), and dried under vacuum at 40-50° C. for 16 hr to afford atazanavir sulfate in Form A (1.04 g, 91% yield, 99.9% HPLC purity).

Provenance & Evidence