An Efficient and Sustainable Synthesis of the Antimalarial Drug Tafenoquine

Abstract

An 11-step, 8-pot synthesis of the antimalarial drug tafenoquine succinate was achieved in 42% overall yield using commercially available starting materials. Compared to the previous manufacturing processes that utilize environmentally egregious organic solvents and toxic reagents, the current route features a far greener (as measured by Sheldon's E Factors) and likely more economically attractive sequence, potentially expanding the availability of this important drug worldwide.