Identification of an isomer impurity in piperaquine drug substance |
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Authors: | Lindegårdh N Giorgi F Galletti B Di Mattia M Quaglia M Carnevale D White N J Mazzanti A Day N P J |
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Institution: | Faculty of Tropical Medicine, Mahidol University, Bangkok 10400, Thailand. niklas@tropmedres.ac |
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Abstract: | A significant contaminant of the antimalarial drug piperaquine (1,3-bis-4-(7-chloroquinolyl-4)-piperazinyl-1]propane) has been identified using liquid chromatography-mass spectrometry (LC-MS) and 2D NMR spectroscopy (1H-1H COSY, 1H-13C HSQC, 1H-13C HMBC). The impurity was identified as the positional isomer 1-(5-chloroquinolin-4)-piperazinyl]-3-(7-chloroquinolin-4)-piperazinyl]propane. The impurity is formed because of contamination of batches of 4,7-dichloroquinoline (a precursor in the synthesis of piperaquine) with 4,5-dichloroquinoline. The amount of impurity (peak area impurity/peak area piperaquine using LC-UV at 347 nm) in old batches of piperaquine and in Artekin (the combination of dihydroartemisinin-piperaquine) ranged from 1.5 to 5%. |
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