Iridium-catalyzed asymmetric reductive amination of C2-acylpyridines

Chiral 1-pyridin-2-yl-ethylamines are significant building blocks for synthetic chemistry and pharmaceutical sciences, while their stereoselective and practical synthesis remains challenging and usually troublesome. Herein, we present a novel iridium-catalyzed direct asymmetric reductive amination of 2-acylpyridines with anilines, affording a series of chiral 1-pyridin-2-yl-ethylamines with up to 97% yield and 95% ee. A 5 mmol scale reaction is also performed to demonstrate the practicality of this method.