Scientia Pharmaceutica is published by MDPI from Volume 84 Issue 3 (2015).
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Sci. Pharm. 2015, 83(3), 445-452; doi:10.3797/scipharm.1501-13 (registering DOI)
Synthesis of Isomeric and Potent Impurities of the Triazole-Based Antifungal Drug Voriconazole
Chemical Research and Development, APL Research Centre-II, Aurobindo Pharma Ltd., Survey No. 71 & 72, Indrakaran (V), Medak Dist.-502329, Andhra Pradesh, India
Department of Engineering chemistry, Andhra University College of Engineering (A), Andhra University, Visakhapatnam-530003, Andhra Pradesh, India
Author to whom correspondence should be addressed.
Received: 25 January 2015 / Accepted: 6 March 2015 / Published: 6 March 2015
Abstract We describe the synthesis of two positional isomers and a desfluoro impurity of Voriconazole starting with Friedel–Crafts acylation of mono- and difluoro-benzene. These isomers are the crucial components in determining the quality of Voriconazole during its manufacturing from the key raw material, 1-(2,4-difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethan-1-one. All the prepared impurities were characterized by IR, 1H-NMR, 13C-NMR, and mass spectral data.
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SUNDARAM, D.T.S.S.; MITRA, J.; ISLAM, A.; PRABAHAR, K.J.; VENKATESWARA RAO, B.; PAUL DOUGLAS, S. Synthesis of Isomeric and Potent Impurities of the Triazole-Based Antifungal Drug Voriconazole. Sci. Pharm. 2015, 83, 445-452.
SUNDARAM DTSS, MITRA J, ISLAM A, PRABAHAR KJ, VENKATESWARA RAO B, PAUL DOUGLAS S. Synthesis of Isomeric and Potent Impurities of the Triazole-Based Antifungal Drug Voriconazole. Scientia Pharmaceutica. 2015; 83(3):445-452.
SUNDARAM, Dhanraj T. S. S.; MITRA, Jayati; ISLAM, Aminul; PRABAHAR, Koilpillai Joseph; VENKATESWARA RAO, Battula; PAUL DOUGLAS, Sanasi. 2015. "Synthesis of Isomeric and Potent Impurities of the Triazole-Based Antifungal Drug Voriconazole." Sci. Pharm. 83, no. 3: 445-452.
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