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Updated: Feb 9, 2026
08:38
Targeted DNA Methylation Analysis by Next-generation Sequencing
Published on: February 24, 2015
38.0K
Selective Methylation of Arenes: A Radical C-H Functionalization/Cross-Coupling Sequence.
Fabien Serpier1, Fei Pan1, Won Seok Ham1,2
1Department Max-Planck-Institut für Kohlenforschung, Kaiser-Wilhelm-Platz 1, 45470, Mülheim an der Ruhr, Germany.
Angewandte Chemie (International Ed. in English)
|June 13, 2018
Summary
A new method enables selective methylation of arenes using C-H functionalization and nickel catalysis. This approach provides efficient access to para-methylated compounds, including for late-stage pharmaceutical modification.
Area of Science:
- Organic Chemistry
- Catalysis
- Synthetic Methodology
Background:
- Direct functionalization of C-H bonds is a key goal in organic synthesis.
- Methylation of aromatic compounds is crucial for modifying molecular properties.
Purpose of the Study:
- To develop a novel, selective, and nonchelation-assisted method for arene methylation.
- To enable rapid access to para-methylated arenes.
Main Methods:
- Combination of C-H functionalization with nickel-catalyzed cross-coupling.
- Development of a selective methylation protocol for arenes.
Main Results:
- Achieved selective, nonchelation-assisted methylation of arenes.
- Demonstrated high para selectivity in the methylation reaction.
- Showcased the utility of the method for late-stage methylation of pharmaceuticals.
Conclusions:
- The developed method offers an efficient route to para-methylated arenes.
- This transformation is valuable for late-stage functionalization in drug discovery.
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