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Updated: Jul 28, 2026

Protocol for the Synthesis of Ortho-trifluoromethoxylated Aniline Derivatives
Published on: January 19, 2016
Synthesis of dimeric trifluoromethoxyacridine-derived pathogen-inactivating nucleic acid intercalators
René Csuk1, Christian Raschke, Gunnar Göthe
1Institut für Organische Chemie, Martin-Luther-Universität Halle-Wittenberg, D-06120 Halle (Saale), Germany. csuk@chemie.uni-halle.de
Abstract:
A series of antiviral active compounds consisting of an intercalating acridine-derived part, a spacer region and a reactive EDTA-derived conjugate was synthesized in an easy sequence. Thus, suitably mono-protected 1,omega-alkyldiamines gave, upon reaction with 9-chloro-2-trifluoromethoxyacridine, followed by deprotection and reaction with EDTA dianhydride, the target molecules. Incorporation of their Fe(II) complexes in the presence of ascorbate gave a reduction of the phage titer of MS2 phages by several logarithmic decades.
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