Optimization and Scaling up of the Azaindole Derivatives Synthesis

Authors

DOI:

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

Keywords:

azaindoles, Sonogashira coupling, Larock synthesis, carbonylation

Abstract

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.

Supporting Agency

  • The author received no specific funding for this work.

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Published

2025-11-21

How to Cite

(1)
Kordubailo, M. V.; Tolmachev, A. A. Optimization and Scaling up of the Azaindole Derivatives Synthesis. J. Org. Pharm. Chem. 2025, 23, 4-10.

Issue

Vol. 23 No. 3 (2025)

Section

Original Researches

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