Synthesis of Isomeric and Potent Impurities of the Triazole-Based Antifungal Drug Voriconazole |
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| Authors: | Dhanraj T. S. S. Sundaram Jayati Mitra Aminul Islam Koilpillai Joseph Prabahar Battula Venkateswara Rao Sanasi Paul Douglas |
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| Affiliation: | 1Chemical Research and Development, APL Research Centre-II, Aurobindo Pharma Ltd., Survey No. 71 & 72, Indrakaran (V), Medak Dist.-502329, Andhra Pradesh, India;2Department of Engineering chemistry, Andhra University College of Engineering (A), Andhra University, Visakhapatnam-530003, Andhra Pradesh, India |
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| Abstract: | We describe the synthesis of two positional isomers and a desfluoro impurity of Voriconazole starting with Friedel–Crafts acylation of mono- and difluorobenzene. 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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| Keywords: | Voriconazole Impurity synthesis Positional isomers Chloroacetyl chloride |
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