作者:R. Ian Storer、Diane E. Carrera、Yike Ni、David W. C. MacMillan
DOI:10.1021/ja057222n
日期:2006.1.1
The first enantioselective organocatalytic reductive amination reaction has been accomplished. The development of a new chiral phosphoric acid catalyst has provided a convenient strategy for the enantioselective construction of protected primary amines and provided a highly stereoselective method for the reductive amination of heterocyclic amines. A diverse spectrum of ketone and amine substrates can
第一个对映选择性有机催化还原胺化反应已经完成。新型手性磷酸催化剂的开发为受保护伯胺的对映选择性构建提供了一种方便的策略,并为杂环胺的还原胺化提供了一种高度立体选择性的方法。可以以高产率和出色的对映选择性容纳各种不同的酮和胺底物。这种新协议实现了还原胺化与亚胺还原的关键优势,因为从烷基-烷基酮衍生的酮亚胺对分离不稳定,使用这种直接有机催化还原胺化可以全面绕过这一基本限制。