Disulfonimide‐Catalyzed Asymmetric Reduction of N‐Alkyl Imines

Abstract A chiral disulfonimide (DSI)‐catalyzed asymmetric reduction of N ‐alkyl imines with Hantzsch esters as a hydrogen source in the presence of Boc 2 O has been developed. The reaction delivers Boc‐protected N ‐alkyl amines with excellent yields and enantioselectivity. The method tolerates a large variety of alkyl amines, thus illustrating potential for a general reductive cross‐coupling of ketones with diverse amines, and it was applied in the synthesis of the pharmaceuticals ( S )‐Rivastigmine, NPS R‐568 Hydrochloride, and ( R )‐Fendiline.