Nickel/Photoredox Dual-Catalyzed Regioselective Alkyl-Aminoalkylation of Alkenes

Abstract Selective alkene dialkylation represents one of the most challenging transformations in alkene difunctionalization reactions. Here, we report an excellent site-selective dialkylation of alkenes via photoredox/nickel dual catalysis. Taking advantage of the synergistic catalytic model, excellent orthogonal substrate activation could be achieved to address otherwise difficult-to-controlled chemo- and regioselectivity issues. Alkyl halides and alkyl tertiary amines are used as mild alkylating reagents, thus bypassing the use of sensitive organometallic reagents. The present strategy shows a broad scope for both alkyl electrophiles and nucleophiles, and provides a facile access to valuable β-amino acid derivatives, which are key structural units among numerous biologically active compounds.