Synthesis of Trifluoromethylthiolated Quinolinones via Trifluoromethanesulfanamide‐Induced Electrophilic Intramolecular Cyclization of N‐Arylpropynamides

Abstract The reaction of N ‐arylpropynamides with the commercially available trifluoromethanesulfanamide in the presence of BiCl 3 was found to afford quinolin‐2‐ones in a selective manner via electrophilic trifluoromethylthiolation enabled by the in‐situ generated CF 3 S−Cl and the followed intramolecular cyclization. Differing from the existing analogous cyclization route that solely produces spiro[4,5]trienones, this alternative approach exclusively affords the biologically interesting quinolin‐2‐ones as the major products.