Abstract

A three-component annulation reaction and trifluoromethylation for the construction of 3-(trifluoromethyl)-4H-pyrans using β-CF3-1,3-enynes, BrCF2CO2Et, and sulfoxonium ylides as readily available substrates has been developed. This metal-free process involves two C-F bond cleavages of β-CF3-1,3-enynes and a CF3 group generated in situ from BrCF2CO2Et. This method is applicable to the late-stage modification of pharmaceutically active molecules.

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