A Strategy to Aminate Pyridines, Diazines, and Pharmaceuticals via Heterocyclic Phosphonium Salts

作者:Patel Chirag; Mohnike Margaret; Hilton Michael C; McNally Andrew*
来源:Organic Letters, 2018, 20(9): 2607-2610.
DOI:10.1021/acs.orglett.8b00813

摘要

A straightforward process to aminate pyridines and diazines is presented 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.

  • 出版日期2018-5-4