In this paper, we provide an overview on atazanavir sulfate, a novel azapeptide protease inhibitor, including the physicochemical properties, crystalline type, synthesis methods for the main intermediates (2R, 3S) -Boc [epoxide (2R, 3S) -3- (tert-butoxycarbonyl) amino- 1, 2-epoxy- 4- phenylbutane)] and the finished product, current market for the active pharmaceutical ingredient and the main intermediates, R&D efforts at home and abroad, and clinical applications for AIDS patients. At the end of the article we also provide a critical analysis of atazanavir sulfate.