posted on 2020-04-01, 19:06authored byCheng-Gang Wang, Rui Wu, Ting-Peng Li, Tao Jia, Yang Li, Dongmei Fang, Xiaozhen Chen, Yuanji Gao, Hai-Liang Ni, Ping Hu, Bi-Qin Wang, Peng Cao
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.