Phosphine/palladium-catalyzed syntheses of alkylidene phthalans, 3-deoxyisoochracinic acid, isoochracinic acid, and isoochracinol

Org Lett. 2012 Jul 6;14(13):3264-7. doi: 10.1021/ol301154f. Epub 2012 Jun 21.

Abstract

In this study we used sequential catalysis-PPh(3)--catalyzed nucleophilic addition followed by Pd(0)-catalyzed Heck cyclization--to construct complex functionalized alkylidene phthalans rapidly, in high yields, and with good stereoselectivities (E/Z ratios of up to 1:22). The scope of this Michael-Heck reaction includes substrates bearing various substituents around the alkylidene phthalan backbone. Applying this efficient sequential catalysis, we accomplished concise total syntheses of 3-deoxyisoochacinic acid, isoochracinic acid, and isoochracinol.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Benzofurans / chemical synthesis*
  • Benzofurans / chemistry
  • Catalysis
  • Molecular Structure
  • Palladium / chemistry*
  • Phosphines / chemistry*
  • Phthalic Acids / chemical synthesis*
  • Phthalic Acids / chemistry
  • Stereoisomerism

Substances

  • 3-deoxyisoochracinic acid
  • Benzofurans
  • Phosphines
  • Phthalic Acids
  • isoochracinic acid
  • isoochracinol
  • Palladium
  • phosphine