Diels-Alder cycloadditions of 5-hydroxy-2-pyrones: 2H-pyran-2,5-diones and 5-(tert-butyldimethylsilyloxy)-2-pyrones as synthons

  • Wanqing Wu
  • , Shuzhong He
  • , Xiongfei Zhou
  • , Chi Sing Lee*
  • *Corresponding author for this work

Research output: Contribution to journalJournal articlepeer-review

14 Citations (Scopus)

Abstract

Diels-Alder (DA) cycloadditions of 5-hydroxy-2-pyrones based on the use of 2H-pyran-2,5-diones and 5-(tert-butyldimethylsilyloxy)-2-pyrones as synthons have been developed. Upon treatment either with a base or with a Lewis acid, 2Hpyran-2,5-diones equilibrated to 5-hydroxy-2-pyrones and underwent DA cycloaddition. The base-catalyzed protocol was optimized with cHex 2NMe (0.1 equiv.) in tBuOH at room temperature, which gave the tricyclic cycloadducts in yields of up to 81% (endo/exo = 6.2:1), The Lewis-acid-promoted protocol was optimized by conversion of 2H-pyran-2,5-diones into 5-(tert-butyldimethylsilyloxy)-2-pyrones and use of BF3· OEt2, which afforded the same DA products in yields of up to 90% (endo/exo = 12:1).

Original languageEnglish
Pages (from-to)1124-1133
Number of pages10
JournalEuropean Journal of Organic Chemistry
Issue number6
DOIs
Publication statusPublished - Feb 2010

User-Defined Keywords

  • 2-Pyrones
  • Cycloaddition
  • Lactones

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