Cu(II)-Mediated C–S/N–S Bond Formation via C–H Activation: Access to Benzoisothiazolones Using Elemental Sulfur

A copper-mediated
C–S/N–S bond–forming reaction
via C–H activation that uses elemental sulfur has been developed.
The addition of TBAI was found to be crucial for the success of this
transformation. The method is scalable, shows excellent functional
group tolerance, and is compatible with heterocycle substrates, providing
efficient and practical access to benzoisothiazolones. The direct
diversification of the benzoisothiazolone products into a variety
of sulfur-containing compounds is also demonstrated.