Organophosphine as an Alkyl Transfer Shuttle for the Direct β-Alkylation of Chalcones Using Alkyl Halides

J Org Chem. 2023 Jan 6;88(1):534-539. doi: 10.1021/acs.joc.2c02505. Epub 2022 Dec 19.

Abstract

We report an efficient alkyl transfer strategy for the direct β-alkylation of chalcones using commercially available alkyl bromides as alkyl reagents. In this transformation, the ortho-phosphanyl substituent in the chalcones is crucial for controlling their reactivity and selectivity. It also serves as a reliable alkyl transfer shuttle to transform electrophilic alkyl bromides into nucleophilic alkyl species in the form of quaternary phosphonium salts and transfer the alkyl group effectively to the β-position of the chalcones. This alkyl transfer strategy can be further extended to the alkenylation of ortho-phosphanyl benzaldehydes to assemble functionalized polyenes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkylation
  • Bromides
  • Catalysis
  • Chalcones*
  • Salts

Substances

  • Chalcones
  • Bromides
  • Salts