Direct synthesis of substituted tetrahydrofurans via regioselective dehydrative polyol cyclization cascades

Amy B. Dounay, Gordon John Florence, Akira Saito, Craig J. Forsyth

Research output: Contribution to journalArticlepeer-review

18 Citations (Scopus)

Abstract

A one-pot procedure for the conversion of 1,2,4,5-tetraols into substituted tetrahydrofuran moieties has been developed. This involves the regioselective sulfonylation of the terminal hydroxyl of the polyol array followed by sequential oxirane and oxolane formation under basic conditions. A survey of reaction conditions has defined the use of N-(2,4,6-triisopropylbenzenesulfonyl)imidazole as sulfonylation reagent, potassium tert-butoxide as base, and tert-butanol as solvent to be optimal. Under these conditions, 8-O-benzyl-octan-1,2,4,5,8-pentaol was converted stereospecifically into tetrahydrofurans in 62% yield. Polyol substrates were derived from Sharpless asymmetric dihydroxylation of 1,4-dienes. Hence, substituted tetrahydrofurans could be obtained stereospecifically from diene substrates in two operations. (C) 2002 Elsevier Science Ltd. All rights reserved.

Original languageEnglish
Pages (from-to)1865-1874
Number of pages10
JournalTetrahedron
Volume58
Issue number10
DOIs
Publication statusPublished - 4 Mar 2002

Keywords

  • tetrahydrofurans
  • cyclization
  • 1,4-dienes
  • ENOLATE CLAISEN REARRANGEMENT
  • ASYMMETRIC DIHYDROXYLATION
  • STEREOCHEMICAL CONTROL
  • NATURAL-PRODUCTS
  • LIGAND CLASS
  • OLEFINS

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