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Tropical Journal of Pharmaceutical Research
Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, Nigeria
ISSN: 1596-5996
EISSN: 1596-9827
Vol. 12, No. 5, 2013, pp. 791-798
Bioline Code: pr13099
Full paper language: English
Document type: Research Article
Document available free of charge

Tropical Journal of Pharmaceutical Research, Vol. 12, No. 5, 2013, pp. 791-798

 en An Efficient, Green Chemical Synthesis of the Malaria Drug, Piperaquine
Fortunak, Joseph MD; Byrn, Stephen R; Dyson, Brandon; Ekeocha, Zita; Ellison, Tiffany; King, Christopher L; Kulkarni, Amol A; Lee, Mindy; Conrad, Chelsea & Thompson, Keeshaloy


Purpose: To provide a robust, efficient synthesis of the malaria drug piperaquine for potential use in resource-poor settings.
Methods: We used in-process analytical technologies (IPAT; HPLC) and a program of experiments to develop a synthesis of piperaquine that avoids the presence of a toxic impurity in the API and is optimized for overall yield and operational simplicity.
Results: A green-chemical synthesis of piperaquine is described that proceeds in 92 – 93 % overall yield. The chemistry is robust and provides very pure piperaquine tetraphosphate salt (> 99.5 %). The overall process utilizes modest amounts (about 8 kg/kg) of 2-propanol and ethyl acetate as the only organic materials not incorporated into the API; roughly 60 % of this waste can be recycled into the production process. This process also completely avoids the formation of a toxic impurity commonly seen in piperaquine that is otherwise difficult to remove.
Conclusion: An efficient synthesis of piperaquine is described that may be useful for application in resource-poor settings as a means of expanding access to and reducing the cost of ACTs.

ACTs; Dihydroartemisinin Piperaquine; Dihydroartemisinin; Green Chemistry; Malaria; Piperaquine

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