DOI: 10.1002/chem.71827 ISSN: 0947-6539
Oxidant‐Free Mechanochemical N‐Arylation of Sulfoximines Using Zero‐Valent Copper Powder and Arylboronic Acid
Tao Fang, Tingting Fan, Cong Chen, Zhixiu Liu, Baodong Cui, Yongzheng Chen, Shiming ZhangABSTRACT
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.