Development and Scale Up of a Fully Continuous Flow Synthesis of 2-Hydroxypyridine-N-Oxide

Time: 3:00 pm
day: Day One


  • A fully continuous-flow synthesis of 2-hydroxypyridine-N-oxide (HOPO), an important peptide coupling reagent used in a variety of pharmaceutical ingredients preparations, was designed, developed, and scaled up
  • The process involves the catalytic oxidation of 2-hydroxypyridine using hydrogen peroxide, followed by quenching and hydrolysis to obtain HOPO in aqueous solution
  • The continuous reaction process and post-treatment process resulted in >90% isolated yield, with no need for additional separation and purification steps, thus avoiding interruption of the continuous reaction. The scale-up process successfully achieved a production rate of 8 kg/day, making this synthesis method highly suitable for industrial applications.