Synthesis of 2-trifluoromethylated quinolines from CF3-alkenes

Org Biomol Chem. 2021 May 21;19(19):4303-4319. doi: 10.1039/d1ob00098e. Epub 2021 Apr 26.

Abstract

α-CF3-enamines can be prepared by the reaction of pyrrolidine with the corresponding haloalkenes. The prepared enamines react with 2-nitrobenzaldehydes to give ortho-nitro-substituted α,β-diaryl-CF3-enones highly stereoselectively in up to 88% yield. Subsequent reduction of the nitro-group by an Fe-AcOH system promotes intramolecular cyclization to afford 2-CF3-3-arylquinolines in up to 99% isolated yield. High synthetic utility of all synthetic steps of the sequence was shown. A one-pot procedure was developed to give the target trifluoromethylated quinolines directly from enamines or haloalkenes.

Publication types

  • Research Support, Non-U.S. Gov't