Copper(I)-Catalyzed Ketenimine Formation/Aza-Claisen Rearrangement Cascade for Stereoselective Synthesis of α-Allylic Amidines
2020
A copper-catalyzed
three-component reaction of terminal alkynes,
TsN3, and tertiary allylic amines is developed toward the
one-pot synthesis of α-allylic amidines. The product was synthesized
on gram scale under 1 mol % of catalyst loading. Transformations of
products into alkenyl amine and other nitrogen-containing compounds
are demonstrated without any loss of stereochemical information.
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