A Convergent Synthetic Study of Biologically Active Benzofuran Derivatives

  • Hu, Kun (College of Pharmacy, Kyung Hee University) ;
  • Jeong, Jin-Hyun (College of Pharmacy, Kyung Hee University)
  • Published : 2006.06.01

Abstract

In order to construct a benzofuran library, we developed a model study of benzbromarone. Synthesis has been achieved in 53% overall yield, starting from phenol via the key intermediate 2-ethylbenzofuran which was afforded by intramolecular Wittig reaction.

Keywords

References

  1. Buu-Hoi, N. P., Bisagni, E., Royer, R., and Routier, C., Oxygen, heterocycles. Part VII. spasmolytic ketones in the benzofuran series, and related compounds. J. Chem. Soc., 625-627 (1957) https://doi.org/10.1039/jr9570000625
  2. Buu-Hoi. N. P., Xuong, and Bac, Oxygen, heterocycles. Part X. the acylation of benzofuran. J. Chem. Soc., 173 (1964)
  3. Elks, J. and Ganellin, C. R., Dictionary of Drugs, Chapman and Hall, 1990, 1st edition
  4. Hercouet, A. and Le Corre, M., Une nouvelle voie daces aux benzofurannes. Tetrahedron Letters, 23, 2145-2148 (1979)
  5. Hercouet, A. and Le Corre, M., Acyloxyalkylidenephosphoranes- III. Etude des ${\omega}$-Acyloxybenzylidenetriphenylphosphoranes. Nouvelle voie Dacces aux benzofurannes. Tetrahedron, 37, 2867-2873 (1981) https://doi.org/10.1016/S0040-4020(01)92357-9
  6. Morozumi, T. and Komiyama, M., Quantitative analysis on ortho-directing activities of divalent metal salts in hydroxymethylation of phenol by formaldehyde. Journal of Molecular Catalysts, 69, 339-346 (1991) https://doi.org/10.1016/0304-5102(91)80114-I
  7. Zhang, D. Y. and Hua, W. Y., Improvement on the synthetic method of Benzbromarone. Jingxi Huagong, 19, 329-331 (2002)