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Published on: June 23, 2019
Environmentally Responsible and Cost-Effective Synthesis of the Antimalarial Drug Pyronaridine
Joseph R A Kincaid1, Rahul D Kavthe1, Juan C Caravez1
1Department of Chemistry & Biochemistry, University of California, Santa Barbara, California 93106 United States.
Abstract:
Two routes to the antimalarial drug Pyronaridine are described. The first is a linear sequence that includes a two-step, one-pot transformation in an aqueous surfactant medium, leading to an overall yield of 87%. Alternatively, a convergent route utilizes a telescoped three-step sequence involving an initial neat reaction, followed by two steps performed under aqueous micellar catalysis conditions affording Pyronaridine in 95% overall yield. Comparisons to existing literature performed exclusively in organic solvents reveal a 5-fold decrease in environmental impact as measured by E Factors.
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