Ligand‐Boosted Copper Catalysis for Air‐Tolerant Methoxylation of (Hetero)aryl Halides With Sodium Methoxide

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An air‐tolerant, simple yet highly efficient copper‐catalyzed methoxylation of (hetero)aryl bromides and some activated chlorides has been developed by using copper(II) chloride/2,2‐bipyridine as catalyst precursor. A wide range of (hetero)aryl bromides and electron‐deficient chlorides could be efficiently methoxylated in good to excellent yields at 1‐mol% catalyst loading albeit showing a functional group compatibility dependent on the electronic properties of aryl ring. Applications of the practical protocol have been demonstrated in multigram synthesis of 3,4,5‐trimethoxytoluene.