Copper-catalyzed ortho-Monofluorination of Aniline Derivatives with Selectfluor Directed by Picolinic Acid Amides

Abstract

A novel and facile method for selective ortho-C―H monofluorination of aniline derivatives was achieved using Selectfluor/Cu(OAc)₂/HOAc system. The reaction proceeded via electrophilic process with diverse substrates in acceptable moderate to high yields. The position selectivity was controlled by bidentate coordination of picolinic acid amides with copper.

Keywords

Monofluorination / Aniline / Selectfluor / Picolinic acid / Copper

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