A Direct Method for Synthesis of Fluorinated Quinazolinones and Quinoxalines Using Fluorinated Acids without Metals or Additives

Abstract

The trifluoromethyl group only exists in synthetic compounds. Owing to the unique bioactivities of this group, the trifluoromethylation of alkanes, arenes, unsaturated compounds like olefins, aldehydes­, and ketones, and heterocycles has been studied constantly in recent decades. Herein, a direct method using trifluoroacetic acid as a CF₃ source for the synthesis of 2-(trifluoromethyl)quinazolin-4-ones and 4-(trifluoromethyl)pyrrolo/indolo[1,2-a]quinoxalines without any catalysts or additives is reported; a wide range of fluorinated compounds were obtained in 52%–94% yield.

Key words

fluorination - trifluoromethyl - quinazolinones - quinoxalines - metal-free - solvent-only

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