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Updated: Jun 21, 2026
07:06
A Microwave-Assisted Direct Heteroarylation of Ketones Using Transition Metal Catalysis
Published on: February 16, 2020
Recent advances in aryl-aryl bond formation by direct arylation
Gerard P McGlacken1, Lorraine M Bateman
1Chemistry Department and Analytical and Biological Chemistry Facility, University College Cork, Ireland. g.mcglacken@ucc.ie
Chemical Society Reviews
|July 23, 2009
Summary
Direct arylation via C-H activation offers an efficient synthetic route to biaryl compounds, reducing steps and waste compared to traditional methods like Suzuki-Miyaura coupling.
Area of Science:
- Organic Chemistry
- Synthetic Chemistry
- Catalysis
Background:
- The biaryl structural motif is prevalent in natural products, pharmaceuticals, and materials.
- Traditional methods for aryl-aryl bond formation, such as Mizoroki-Heck and Suzuki-Miyaura reactions, are well-established.
- These traditional methods often require prefunctionalization of starting materials, adding steps and generating waste.
Purpose of the Study:
- To review recent advancements in aryl-aryl bond formation.
- To highlight direct arylation via C-H activation as a key alternative methodology.
- To cover literature reports from January 1, 2006, to October 22, 2008.
Main Methods:
- Focus on direct arylation strategies targeting C-H bonds.
- Comparison with established cross-coupling reactions.
- Analysis of literature data within a specified timeframe.
Main Results:
- Direct arylation provides biaryls in fewer synthetic steps.
- C-H activation methods minimize the need for prefunctionalization.
- This methodology offers reduced waste and improved atom economy.
Conclusions:
- Direct arylation via C-H activation is a powerful and increasingly important strategy for synthesizing biaryl compounds.
- This approach offers significant advantages over traditional cross-coupling methods in terms of efficiency and sustainability.
- The reviewed period showcases substantial progress in this field.
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