Last Decade of Unconventional Methodologies for the Synthesis of Substituted Benzofurans

Molecules. 2020 May 16;25(10):2327. doi: 10.3390/molecules25102327.

Abstract

This review describes the progress of the last decade on the synthesis of substituted benzofurans, which are useful scaffolds for the synthesis of numerous natural products and pharmaceuticals. In particular, new intramolecular and intermolecular C-C and/or C-O bond-forming processes, with transition-metal catalysis or metal-free are summarized. (1) Introduction. (2) Ring generation via intramolecular cyclization. (2.1) C7a-O bond formation: (route a). (2.2) O-C2 bond formation: (route b). (2.3) C2-C3 bond formation: (route c). (2.4) C3-C3a bond formation: (route d). (3) Ring generation via intermolecular cyclization. (3.1) C7a-O and C3-C3a bond formation (route a + d). (3.2) O-C2 and C2-C3 bond formation: (route b + c). (3.3) O-C2 and C3-C3a bond formation: (route b + d). (4) Benzannulation. (5) Conclusion.

Keywords: inter-molecular approach; intra-molecular approach; synthesis of benzofurans.

Publication types

  • Historical Article
  • Review

MeSH terms

  • Benzofurans / chemical synthesis*
  • Benzofurans / chemistry
  • Biological Products / chemical synthesis*
  • Biological Products / chemistry
  • Catalysis
  • Chemistry Techniques, Synthetic / history
  • Chemistry Techniques, Synthetic / methods*
  • Chemistry, Pharmaceutical / history
  • Chemistry, Pharmaceutical / methods
  • Cyclization
  • History, 21st Century
  • Humans
  • Pharmaceutical Preparations / chemical synthesis*
  • Pharmaceutical Preparations / chemistry

Substances

  • Benzofurans
  • Biological Products
  • Pharmaceutical Preparations