First Safe and Practical Synthesis of 2-Amino-8-hydroxyquinoline

Abstract

The first safe and efficient synthesis of the important building block 2-amino-8-hydroxyquinoline (1) is described. Starting from the readily available N-oxide 3 of the cheap bulk chemical 8-hydroxyquinoline (2), the target compound is obtained in a two-step one pot procedure in good overall yield (53−66%) and purity (>98%) on a kilogram scale without chromatography.