Asymmetric copper-catalyzed propargylic amination with amine hydrochloride salts?

Chemical Communications Pub Date: 2021-04-07 DOI: 10.1039/D1CC00663K

Abstract

The highly enantioselective copper-catalyzed propargylic amination of propargylic esters with amine hydrochloride salts has been realized for the first time using copper salts with chiral N,N,P-ligands. This method features a broad substrate scope and wide functional group tolerance, generating propargylic amines in good to excellent yields with high enantioselectivities (up to 99% ee). The utility of the approach was demonstrated by late-stage functionalization of marketed pharmaceuticals.

Graphical abstract: Asymmetric copper-catalyzed propargylic amination with amine hydrochloride salts
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