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Merging photoredox/nickel catalysis enabling the cross-electrophile coupling of aziridines with pyridin-1-ium salts involving dearomatization for the synthesis of β-(1,4-dihydropyridin-4-yl)-ethylamines, especially including bioactive motif-based analogues, is described. This method allows incorporation of a 1,4-dihydropyridin-4-yl group and formation a N-H amino group to construct highly valuable β-(1,4-dihydropyridin-4-yl)-ethylamine frameworks in a single step through the C2-N bond regioselective cleavage and dearomatization alkylati