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The regioselective synthesis of α,β-difunctionalized (alkenyl, aryl, sulfonyl, allyl, or alkynyl) azepenes has been accomplished through α-halo eneformamides. A successful implementation of the vicinal functionalization strategy has led to a one-pot synthesis of 2-benzazepanes whose benzenoid portion is highly functionalized.

Graphical abstract: Expedient access to α,β-difunctionalized azepenes using α-halo eneformamides: application to the one-pot synthesis of 2-benzazepanes

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