Disulfonimide‐Catalyzed Asymmetric Reduction of
<i>N</i>
‐Alkyl Imines
作者:Vijay N. Wakchaure、Philip S. J. Kaib、Markus Leutzsch、Benjamin List
DOI:10.1002/anie.201504052
日期:2015.9.28
A chiral disulfonimide (DSI)‐catalyzed asymmetric reduction of N‐alkyl imines with Hantzsch esters as a hydrogen source in the presence of Boc2O 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
在Boc 2 O存在的情况下,已开发出一种以Hantzsch酯为氢源的手性二磺酰亚胺(DSI)催化N烷基亚胺的不对称还原。该反应可提供具有出色收率和对映选择性的Boc保护的N-烷基胺。该方法可耐受多种烷基胺,从而说明了酮与各种胺的一般还原性交叉偶联的潜力,并已用于药物(S)-利伐斯的明,NPS R-568盐酸盐的合成,以及(R)-芬迪林。