Synthesis of Thiaphenanthridinones from Sulfinate Esters and 2-Borylanilines

A facile palladium-catalyzed synthesis of thiaphenanthridinones from sulfinate esters and 2-borylanilines is disclosed. Various sulfur analogs of phenanthridinones were synthesized by bromide-selective cross-coupling and cyclization in one step. Further transformations of the obtained thiaphenanthridinones allowed preparing a broad range of thiaphenanthridinone derivatives involving analogs of bioactive compounds.