Benzofuran derivatives are actively investigated in the therapy of the Alzheimer disease¹. We have prepared two new fluorinated benzofuran derivatives².

The syntheses started with the preparation and reduction of 2-(4-nitrophenyl)benzofuran to the corresponding amine. The amine was transformed into hydroxy group via diazonium salt. Etherification, followed by the Friedel-Crafts acylation with 4-trifluoromethylbenzoyl chloride and 2-fluorobenzoyl chloride, completed the syntheses. The fluorinated products are potential inhibitors of β-amyloid aggregation, and might be tested in the Alzheimer disease therapy.

1) Rizzo S., Riviére C., Piazzi L., Bisi A., Gobbi S., Bartolini M., Andrisano V., Morroni F., Tarozzi A.,  Monti J.-P., Rampa A., J. Med. Chem., 2008, 51, 2883.

2) M. Zaidlewicz, T. Kosmalski, T. Sengupta, K. P. Mohanakumar, K. Staszak.  „Synthesis of Fluorinated 2,3-Disubstituted Benzofurans Potential β-Amyloid Aggregation Inhibitors”. Heterocycles, 2010, 80, 663-668.

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