A simple, ligand-free Cu(OH)2-catalyzed methoxylation of aryl halides

TL;DR

A new, simple, and cost-effective method for adding methoxy groups to aryl halides using copper hydroxide is developed, useful for chemical labeling.

Contribution

A ligand-free, microwave-assisted methoxylation method using Cu(OH)₂ is introduced for functionalizing aryl halides.

Findings

The method provides synthetically useful yields for methoxylation of aryl halides.

Isotopic labeling with 13C at the methoxy group was successfully demonstrated.

The method does not consistently improve yields in more substituted systems.

Abstract

To develop a simple, rapid and cheap catalytic method for methoxylation of aryl halides for late-stage functionalization and demonstrate its utility in isotopic labelling.

A ligand-free, microwave-assisted method for methoxylation of aryl halides using copper(II) hydroxide as catalyst has been explored. The new method is simple and cheap, afforded synthetically useful yields in some cases, but does not seem to give generally higher yields in more substituted systems. The viability of isotopic labelling using the method has been demonstrated by 13C-incorporation at the methoxy group.

The online version contains supplementary material available at 10.1186/s13104-026-07720-x.

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