Catalyst-Free, Heating-Induced Desulfurization Annulation of CF3-Imidoyl Sulfoxonium Ylides with Isothiocyanates for the Synthesis of 2-Trifluoromethyl-4-aminoquinolines

A heating-induced desulfurization annulation of readily available CF3-imidoyl sulfoxonium ylides and isothiocyanates for the construction of 2-trifluoromethylquinolines has been achieved. The developed transformation was performed under metal- and additive-free conditions, producing a variety of biologically valuable 2-trifluoromethylquinoline derivatives with high efficiency.

Automated summary

A heating-induced desulfurization annulation of CF3-imidoyl sulfoxonium ylides and isothiocyanates has been developed for the synthesis of 2-trifluoromethylquinolines. The reaction proceeds under metal- and additive-free conditions, providing various biologically valuable derivatives with high efficiency.