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An iron-catalyzed dearomative amination of β-naphthols via a nitrene-transfer process has been developed. Oxadiazolones, which have rarely been applied for the synthesis of amidines, are used as the nitrene source. A variety of amidines bearing β-naphthalenone moieties were generated smoothly in good to high yields (up to 98%) in the presence of 1.5 equivalents of tetrabutylammonium bromide, which was added as an essential additive.

Graphical abstract: Synthesis of amidines via iron-catalyzed dearomative amination of β-naphthols with oxadiazolones

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