A Unique Route to Tetrasubstituted Propargylic Amines by Catalytic Markovnikov Hydroamination–Alkynylation

Abstract

Abstract Tetrasubstituted propargylic amines are not accessible from ketones under the many catalytic conditions reported for the synthesis of trisubstituted propargylic amines by reacting an aldehyde with an amine and alkyne. The first tandem Markovnikov hydroamination–alkynylation provides direct access to tetrasubstituted propargylic amines from an amine and alkyne via an unusual route involving no carbonyl compounds. A simple copper salt enables both catalytic cycles without ligands, promoters, co‐catalysts, solvents, or by‐products. magnified image