This article is cited in 1 paper

Communications

Synthesis of novel 8-nitro-substituted 1,3-benzothiazin-4-ones

E. V. Nosova^ab, O. A. Batanova^b, G. N. Lipunova^ab, V. N. Charushin<sup>ab

a</sup> I.Ya. Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences, Ekaterinburg, Russian Federation
^b Institute of Chemical Engineering, Ural Federal University, Ekaterinburg, Russian Federation

Abstract: New 2,5-bis(azacyclohex-1-yl)-8-nitro-1,3-benzothiazin-4-ones were synthesized from 2,6-difluorobenzoic acid in two preparative stages. The ethoxycarbonylpiperazino derivative surpasses in tuberculostatic activity (MIC 4μgml⁻¹) its 5-fluoro-8-H-counterpart. The first representative of 5-fluoro-8-nitro-1,3-benzothiazin-4-ones was obtained through the condensation of 2,6-difluoro-3-nitrobenzoyl isothiocyanate and N-methylindole.

Keywords: 1,3-benzothiazin-4-ones, nitro compounds, benzoyl isothiocyanates, heterocyclization, amino defluorination, organofluorine compounds, tuberculostatic activity.

Language: English

DOI: 10.1016/j.mencom.2020.07.007

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