Login / Signup

A Synthesis of "Dual Warhead" β-Aryl Ethenesulfonyl Fluorides and One-Pot Reaction to β-Sultams.

Praveen K ChinthakindiKimberleigh B GovenderA Sanjeeva KumarHendrik G KrugerThavendran GovenderTricia NaickerPer I Arvidsson
Published in: Organic letters (2017)
Herein, we report an operationally simple, ligand- and additive-free oxidative boron-Heck coupling that is compatible with the ethenesulfonyl fluoride functional group. The protocol proceeds at room temperature with chemoselectivity and E-isomer selectivity and offers facile access to a wide range of β-aryl/heteroaryl ethenesulfonyl fluorides from commercial boronic acids. Furthermore, we demonstrate a "one-pot click" reaction to directly transform the products to aryl-substituted β-sultams.
Keyphrases
  • room temperature
  • ionic liquid
  • randomized controlled trial
  • molecular docking
  • quantum dots
  • structural basis