Darunavir and Atazanavir are two Protease Inhibitors important for the treatment of symptomatic HIV/AIDS. The critical synthetic motif of each is the establishment of two adjacent chiral centers with control of relative and absolute stereochemistry. Small organic ligands are increasingly being used as catalysts to provide such synthetic control via the aldol, Henry, and related reactions. We will report on novel chemistry to achieve new, less expensive syntheses of these molecules with a consequent potential impact on increasing access to these drugs in Less-Developed Countries.

Novel synthesis of darunavir and atazanavir

243rd National Meeting (2012)

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