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Nickel-Catalyzed β‑Regioselective Amination/Cyclization of Ynamide-Nitriles with Amines: Synthesis of Functionalized 3‑Aminoindoles and 4‑Aminoisoquinolines

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posted on 2021-02-03, 15:07 authored by Xiaoping Hu, Xin Xie, Yi Gan, Gaonan Wang, Yuanhong Liu
A highly regioselective nickel/Lewis acid catalyzed amination/cyclization of ynamide-nitriles with amines involving β-addition has been developed. The reaction offers an attractive and efficient route for the synthesis of 3-aminoindoles and 4-aminoisoquinoline derivatives. The Ts-group on the ynamide acts as a directing group to produce the alkenyl nickel species with high regioselectivity.

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