Lipase-catalyzed chemo- and enantioselective acetylation of 2-alkyl/aryl-3-hydroxypropiophenones

Bioorg Med Chem. 2001 Oct;9(10):2643-52. doi: 10.1016/s0968-0896(01)00184-5.

Abstract

The chemo- and enantioselective capabilities of porcine pancreatic lipase (PPL) in tetrahydrofuran, and Candida rugosa lipase (CRL) in diisopropyl ether have been investigated for the acetylation of racemic 2-alkyl/aryl-3-hydroxypropiophenones, which are important precursors in the synthesis of biologically active chromanones and isoflavanones. A highly chemoselective acetylation of primary hydroxy group in preference to phenolic hydroxy group leading to the formation of enantiomerically enriched monoacetates has been observed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetates / chemistry
  • Acetylation
  • Animals
  • Candida / enzymology*
  • Catalysis
  • Chromans / chemistry
  • Chromatography, High Pressure Liquid
  • Crystallography, X-Ray
  • Hydroxylation
  • Hydroxypropiophenone / analogs & derivatives
  • Hydroxypropiophenone / chemistry
  • Hydroxypropiophenone / metabolism*
  • Isoflavones / chemistry
  • Lipase / metabolism*
  • Magnetic Resonance Spectroscopy
  • Models, Chemical
  • Molecular Conformation
  • Molecular Structure
  • Pancreas / enzymology
  • Stereoisomerism
  • Structure-Activity Relationship
  • Substrate Specificity
  • Swine

Substances

  • 3-hydroxy-1-(2-hydroxy-3,4-dimethoxyphenyl)-2-methylpropanone
  • Acetates
  • Chromans
  • Isoflavones
  • Hydroxypropiophenone
  • Lipase