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Synthesis of 2-Amino-8-hydroxyquinoline

The first safe and efficient synthesis of the important building block 2-amino-8-hydroxyquinoline is described.

Tuesday, 31 March 2020

The first safe and efficient synthesis of the important building block 2-amino-8-hydroxyquinoline is described. Starting from the readily available N-oxide 3 of the cheap bulk chemical 8-hydroxyquinoline, 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.