Vol. 23 No. 3 (2025): Issue in Progress

Original Researches

• Optimization and Scaling up of the Azaindole Derivatives Synthesis

  Mykyta V. Kordubailo, Andrey A. Tolmachev

  4-10

  In this study, an optimized method for the synthesis of azaindoles was developed and successfully scaled up to a 100 g batch. Improved yields were observed when using electron-deficient azaheterocycles and substrates bearing electron-withdrawing substituents. 6-Chloro-1H-pyrrolo[3,2-c]pyridine was selected for further functionalization using a carbonylation protocol involving carbon monoxide. As a result, novel and promising building blocks for medicinal chemistry were obtained.

  DOI: https://doi.org/10.24959/ophcj.25.323307

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