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Synthesis and tuberculostatic activity of fluorine-containing derivatives of quinolone, quinazolinone, and benzothiazinone

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Abstract

Methods for the synthesis of fluorine-containing derivatives of quinolones, quinazolinones, and benzothiazinones based on the interaction of polyfluorobenzoic acid chloranhydrides with N,N-N,C-, and N,S-dinucleophiles are described. Use of (tetrafluorobenzoyl)isothiocyanate as the fluorine-containing block provides extensive opportunities for the synthesis of 2-substituted benzothiazinones. Some of the fluorine-containing azaheterocyclic compounds synthesized here had moderate and high activity against Mycobacterium tuberculosis H37Rv.

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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 42, No. 4, pp. 14–18, April, 2008.

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Nosova, É.V., Liponova, G.N., Kravchenko, M.A. et al. Synthesis and tuberculostatic activity of fluorine-containing derivatives of quinolone, quinazolinone, and benzothiazinone. Pharm Chem J 42, 169–174 (2008). https://doi.org/10.1007/s11094-008-0083-0

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  • DOI: https://doi.org/10.1007/s11094-008-0083-0

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