One-pot synthesis of tri- and di-fluoromethylated bis(indolyl)methanols via Friedel-Crafts-type acylation and alkylation

Org Biomol Chem. 2022 Sep 28;20(37):7491-7498. doi: 10.1039/d2ob01281b.

Abstract

A simple and efficient methodology for the first synthesis of tri- and di-fluoromethyl-bis(indolyl)methanols has been demonstrated through a one-pot Friedel-Crafts-type acylation-alkylation of readily available indoles and fluorinated acids. This simple protocol was successfully performed under metal-, additive-, toxic-solvent-, and protective-gas-free conditions, and delivered a wide range of tri- and di-fluoromethyl-bis(indolyl)methanols in moderate to high yields. Notably, this reaction can tolerate diverse vital and reactive functional groups. Furthermore, this one-pot Friedel-Crafts-type acylation-alkylation can be readily expanded to the gram scale with no obvious decrease in the yield, demonstrating its high application potential.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acylation
  • Alkylation
  • Catalysis
  • Indoles*
  • Methanol*
  • Solvents
  • Stereoisomerism

Substances

  • Indoles
  • Solvents
  • Methanol