作者:Michael U. Luescher、Cam-Van T. Vo、Jeffrey W. Bode
DOI:10.1021/ol500210z
日期:2014.2.21
Substituted piperazines and morpholines are valuable structural motifs in biologically active compounds, but are not easily prepared by contemporary cross-coupling approaches. In this report, we introduce SnAP reagents for the transformation of aldehydes into N-unprotected piperazines and morpholines. This approach offers simple, mild conditions compatible with aromatic, heteroaromatic, aliphatic,
取代的哌嗪和吗啉是生物活性化合物中有价值的结构基序,但是用当代的交叉偶联方法不容易制备。在本报告中,我们介绍了SnAP试剂,用于将醛转化为N-未保护的哌嗪和吗啉。该方法可提供与芳族,杂芳族,脂族和乙醛醛兼容的简单温和条件,并在一个步骤中提供单取代和二取代的N-杂环。