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One-Pot Synthesis of Metastable 2,5-Dihydrooxepines through Retro-Claisen Rearrangements: Method and Applications

  • Wei Zhang
  • , Emmanuel Baudouin
  • , Marie Cordier
  • , Gilles Frison
  • , Bastien Nay

Research output: Contribution to journalArticlepeer-review

Abstract

A one-pot methodology to synthesize metastable bicyclic 2,5-dihydrooxepines from cyclic 1,3-diketones and 1,4-dibromo-2-butenes through the retro-Claisen rearrangement of syn-2-vinylcyclopropyl diketone intermediates is reported. DFT calculations were performed to understand the reaction selectivity and mechanisms towards [1,3]- or [3,3]-sigmatropic rearrangements, highlighting the crucial influence of the temperature. The reaction was successfully applied to a short protecting group-free total synthesis of radulanin A, a natural 2,5-dihydrobenzoxepine. Moreover, the strong herbicidal potential of this natural product is demonstrated for the first time.

Original languageEnglish
Pages (from-to)8643-8648
Number of pages6
JournalChemistry - A European Journal
Volume25
Issue number36
DOIs
Publication statusPublished - 26 Jun 2019

Keywords

  • 2,5-dihydrooxepines
  • density functional calculations
  • herbicides
  • sigmatropic rearrangement
  • total synthesis

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