Phenylboronic acid mediated triple condensation reactions of phloroglucinol and unsaturated carbonyl compounds

Org Lett. 2005 Feb 3;7(3):467-70. doi: 10.1021/ol047578o.

Abstract

[reaction: see text] A remarkable phenylboronic acid mediated triple condensation reaction of phloroglucinol (1,3,5-trihydroxybenzene) with a series of alpha,beta-unsaturated carbonyl compounds is reported. This experimentally simple reaction afforded novel C3-symmetric 2H-chromene derivatives. These derivatives represent structural analogues of the natural product xyloketal A, which has been reported to be a potent inhibitor of acetylcholine esterase.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylcholinesterase / metabolism
  • Benzopyrans / chemistry
  • Boronic Acids / chemistry*
  • Catalysis
  • Cholinesterase Inhibitors / chemical synthesis
  • Cholinesterase Inhibitors / pharmacology
  • Phloroglucinol / chemical synthesis*
  • Phloroglucinol / pharmacology
  • Pyrans / chemistry

Substances

  • Benzopyrans
  • Boronic Acids
  • Cholinesterase Inhibitors
  • Pyrans
  • xyloketal A
  • Phloroglucinol
  • Acetylcholinesterase
  • benzeneboronic acid