Recent Progress Concerning the N-Arylation of Indoles
Petr Oeser1, Jakub Koudelka1, Artem Petrenko1
1Department of Organic Chemistry, University of Chemistry and Technology, 16628 Prague, Czech Republic.
Molecules (Basel, Switzerland)
|August 27, 2021
Summary
This review covers modern methods for synthesizing N-arylindoles. It details transition-metal-free, nickel-, palladium-, and copper-catalyzed reactions, highlighting biologically active N-arylindole applications.
Area of Science:
- Organic Chemistry
- Medicinal Chemistry
Background:
- N-arylindoles are crucial scaffolds in medicinal chemistry.
- Efficient synthesis of N-arylindoles is essential for drug discovery.
Purpose of the Study:
- To review and summarize state-of-the-art N-arylation procedures for indoles.
- To highlight recent advancements in the synthesis of biologically active N-arylindoles.
Main Methods:
- Discussion of transition-metal-free N-arylation methods.
- Review of nickel-, palladium-, and copper-catalyzed N-arylation techniques.
Main Results:
- Comprehensive overview of diverse N-arylation strategies.
- Focus on catalytic systems for efficient indole N-arylation.
Conclusions:
- Multiple catalytic and non-catalytic methods exist for N-arylindole synthesis.
- Emerging research focuses on the biological activity of N-arylindole derivatives.
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