Department of Chemistry , Colorado State University , Fort Collins , Colorado 80523 , United States.
Org Lett. 2018 May 4;20(9):2607-2610. doi: 10.1021/acs.orglett.8b00813. Epub 2018 Apr 17.
A straightforward process to aminate pyridines and diazines is presented by reacting phosphonium salt derivatives with sodium azide. The iminophosphorane products are versatile precursors to several nitrogen-containing functional groups, and the process can be applied to building block heterocycles, to drug-like fragments, and for late-stage functionalization of complex pharmaceuticals. Appealing features of this strategy include using C-H bonds as precursors, precise regioselectivity, and a distinct scope from other amination methods, particularly those relying on halogenated azaarenes.
本文提出了一种将磷盐衍生物与叠氮化钠反应来实现吡啶和哒嗪氮原子官能团化的简洁方法。亚磷酰胺产物是多种含氮官能团的多功能前体，该方法可用于砌块杂环、药物样片段以及复杂药物的后期功能化。该策略的吸引人之处包括使用 C-H 键作为前体、精确的区域选择性以及与其他胺化方法（尤其是依赖卤代氮杂芳烃的方法）相比具有明显的优势。
