A short synthesis of Dronedarone

Bioorg Med Chem. 2018 Aug 7;26(14):4330-4335. doi: 10.1016/j.bmc.2018.03.041. Epub 2018 Mar 28.

Abstract

A modification of the Nenitzescu reaction was used to obtain Dronedarone from quinonimine 20 and 1,3-diketone 14 (R = CH2CH2CH2NBu2) in a two-stage process in almost 55% overall yield. Our results represent significant improvement over other state-of-the-art methods as no extra steps for the decoration of the benzofuran core are required.

Keywords: Dronedarone; Nenitzescu; Optimization; Quinonimine.

MeSH terms

  • Benzofurans / chemistry
  • Dronedarone / chemical synthesis*
  • Dronedarone / chemistry
  • Ketones / chemistry
  • Molecular Structure
  • Quinones / chemistry

Substances

  • Benzofurans
  • Ketones
  • Quinones
  • Dronedarone
  • benzofuran