Department of Chemistry, The Pennsylvania State University, University Park, Pennsylvania 16802, USA.
Org Lett. 2011 Sep 16;13(18):4850-3. doi: 10.1021/ol201930e. Epub 2011 Aug 19.
A highly efficient and generally applicable method has been developed to functionalize the ortho-C(sp(2))-H bonds of picolinamide (PA)-protected benzylamine substrates with a broad range of β-H-containing alkyl halides. Sodium triflate has been identified as a critical promoter for this reaction system. The PA group can be easily installed and removed under mild conditions. This method provides a new strategy to prepare highly functionalized benzylamines for the synthesis of complex molecules.
已开发出一种高效且普遍适用的方法，可将吡啶甲酰胺（PA）保护的苄胺底物的邻-C(sp(2))-H 键与广泛的含β-H 的卤代烷基官能化。发现三氟甲磺酸钠是该反应体系的关键促进剂。PA 基团可以在温和的条件下轻松安装和去除。该方法为合成复杂分子的高官能化苄胺提供了一种新策略。
