Recent Developments in C−H functionalisation of Benzofurans and Benzothiophenes

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Abstract

Benzofurans and benzothiophenes are important pharmaceutical motifs, appearing in a broad range of small molecule therapeutic classes. Often overlooked by synthetic methodologists in favour reactions of the analogous indole bicyclic system, there is nevertheless a plurality of approaches to effecting benzofuran and benzothiophene C−H functionalisations. In this review, we summarise progress in this area over the past five years, including 1) alkylations, 2) arylations and heteroarylations, 3) carboxylations, carbamoylations, and C-heteroatom bond formations and 4) cyclisations.

Original languageEnglish
JournalEuropean Journal of Organic Chemistry
Early online date4 Dec 2020
DOIs
Publication statusE-pub ahead of print - 4 Dec 2020

Keywords

  • Benzofuran
  • Benzothiophene
  • Functionalization
  • Heterocycles
  • Synthetic methods

ASJC Scopus subject areas

  • Physical and Theoretical Chemistry
  • Organic Chemistry

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