Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry and Computational Chemistry

Abstract

Synthesis and characterization of Novel Related Substances of Lumefantrine, an anti-malarial drug

Author(s): Madhuresh Kumar Sethi, Anantavena Rani Gonuguntla, Siva Lakshmi Devi Arikatla, Suryanarayana Mulukutla, Rajakrishna Yerramalla, Jaganmohanarao Bontalakoti, Lakshminarayana Vemula and Jayaprakash Thirunavukarasu

Structural characterization related substances of Lumefantrine using IR, NMR data (1H & 13C NMR & MS). During the process development of Lumefantrine, a known antimalarial drug, six related substances were identified. All the six impurities were subsequently synthesized and characterized by IR, NMR and MS spectral data. The six related substances are known as 1-[(9Z)-2,7-dichloro-9-(4-chlorobenzylidene)-9H-fluoren-4-yl]-2-(diethylamino)ethanol 6, 2-(butylamino)-1-[(9Z)-2,7-dichloro-9-(4-chloro benzylidene)-9H-fluoren-4-yl]ethanol 7, 2,7-dichloro-4-[2-(dibutyl amino)-1-hydroxyethyl]-9H-fluoren-9-one 8, 1-[(9Z)-9-benzylidene-2,7-dichloro-9H-fluoren-4-yl]-2-(dibutylamino) ethanol 9, 2-(dibutylamino)-1-[(9Z)-2,7-dichloro-9-(3-chlorobenzylidene)-9H-fluoren-4-yl]ethanol 10, and 2- (dibutylamino)-1-[(9Z)-2,7-dichloro-9-(2-chlorobenzylidene)-9H-fluoren-4-yl]ethanol 11. The present work describes the formation, synthesis and characterization of these impurities. By controlling these new six process related substances will make this high doses anti-malarial drug safer for human use


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