Synthesis of Isomeric and Potent Impurities of the Triazole-Based Antifungal Drug Voriconazole

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-...

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Detalles Bibliográficos
Autores principales: Sundaram, Dhanraj T. S. S., Mitra, Jayati, Islam, Aminul, Prabahar, Koilpillai Joseph, Venkateswara Rao, Battula, Paul Douglas, Sanasi
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Austrian Journal of Pharmaceutical Sciences 2015
Materias:
Research Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4727777/
https://www.ncbi.nlm.nih.gov/pubmed/26839829
http://dx.doi.org/10.3797/scipharm.1501-13
Descripción
Sumario: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, (1)H-NMR, (13)C-NMR, and mass spectral data.

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