Oxidant-Free Mechanochemical N-Arylation of Sulfoximines Using Zero-Valent Copper Powder and Arylboronic Acid.

The N-alkylation of sulfoximines provides an important strategy for the structural modification of drug molecules. However, the synthesis of these compounds generally lacks a convenient protocol and often relies on harsh conditions involving expensive noble metals, toxic solvents, or external oxidants. In this context, we herein propose a sustainable alternative: a mechanochemical activation of zero-valent copper powder via ball milling, which enables an oxidant-free C-N coupling reaction between arylboronic acids and sulfoximines. This method features broad substrate compatibility, straightforward scalability, and the use of recyclable copper powder that retains high activity after recovery.