Electrochemical sulfonylation/Truce-Smiles rearrangement of -allylbenzamides: toward sulfone-containing β-arylethylamines and Saclofen analogues.

The β-arylethylamine pharmacophore is commonly found in medications for central nervous system disorders, prompting the need for safe and efficient methods to endow this motif with relevant functional groups for drug discovery. In this context, herein, we have established electrochemical radical sulfonylation reactions of -allylbenzamides followed by Truce-Smiles rearrangement to produce sulfone- and sulfonate ester-containing β-arylethylamines. Electricity enables this transformation to occur under mild and oxidant-free conditions.