2‑Aminopyridines via Reaction of Pyridine N‑Oxides and Activated Isocyanides

A practical and efficient method for the synthesis of substituted 2-aminopyridines from pyridine N-oxides is reported. Yields of purified, isolated products of up to 84% are observed for the one-pot, two-step process. The reaction involves an in situ deprotection of an isolable N-formylaminopyridine intermediate and facilitates the synthesis of 2-aminopyridines for which other methods fail.

本研究报道了一种以吡啶N-氧化物（pyridine N-oxides）为起始原料合成取代2-氨基吡啶（2-aminopyridines）的实用高效方法。该一锅法两步反应的纯化分离产物收率最高可达84%。反应过程涉及对可分离得到的N-甲酰基氨基吡啶（N-formylaminopyridine）中间体进行原位脱保护，可实现其他合成方法难以完成的2-氨基吡啶类化合物的合成。