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New Fluorine-Containing Derivatives of 4-Anilino-2-(methylsulfanyl)quinazolines

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Abstract

A number of new 4-anilinoquinazolines were synthesized starting from 6,7,8-trifluoro-2-(methyl­sulfanyl)quinazolin-4(3H)-one. Reactions of the title compounds with cyclic secondary amines involved substitu­tion of the 7-fluorine atom with retention of the methylsulfanyl group on C2. 6,7,8-Trifluoro-4-(2-me­thoxyanilno)-2-(methylsulfanyl)quinazoline showed in vitro tuberculostatic activity with a minimum inhibitory concentration of 1.5 μg/mL.

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ACKNOWLEDGMENTS

The authors especially thank M.A. Kravchenko (Ural Research Institute of Phthisiopulmonology, Ministry of Health of the Russian Federation) for performing antituber­cular assays.

Funding

This study was performed under financial support by the Ministry of Science and Higher Education of the Russian Federation [project no. FEUZ-2020-0058 (N687.42B.223/20)].

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Authors and Affiliations

  1. Organic and Biomolecular Chemistry Department, Yeltsin Ural Federal University, 620002, Yekaterinburg, Russia

    E. V. Nosova, Yu. V. Permyakova & V. N. Charushin

  2. Postovsky Institute of Organic Synthesis, Ural Branch, Russian Academy of Sciences, 620219, Yekaterinburg, Russia

    E. V. Nosova, G. N. Lipunova & V. N. Charushin

Authors
  1. E. V. Nosova
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  2. Yu. V. Permyakova
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  3. G. N. Lipunova
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  4. V. N. Charushin
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Corresponding author

Correspondence to E. V. Nosova.

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The authors declare the absence of conflict of interest.

Additional information

Translated from Zhurnal Organicheskoi Khimii, 2021, Vol. 57, No. 3, pp. 437–441 https://doi.org/10.31857/S0514749221030137.

The data of this study were reported at the IVth Int. Conf. “Modern Synthetic Methodologies for the Design of Drugs and Functional Materials” held in Yekaterinburg on November 16–20, 2020.

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Nosova, E.V., Permyakova, Y.V., Lipunova, G.N. et al. New Fluorine-Containing Derivatives of 4-Anilino-2-(methylsulfanyl)quinazolines. Russ J Org Chem 57, 479–482 (2021). https://doi.org/10.1134/S1070428021030222

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  • DOI: https://doi.org/10.1134/S1070428021030222

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