Synthetic and novel biocatalytic resolution studies on (+/-)-5/6/7-acetoxy-4-aryl-3,4-dihydrocoumarins

Bioorg Med Chem. 2003 Feb 20;11(4):529-38. doi: 10.1016/s0968-0896(02)00454-6.

Abstract

Eleven (+/-)-5/6/7-acetoxy-4-aryl-3,4-dihydrocoumarins have been synthesised in two steps starting from the coupling of cinnamic acid/substituted cinnamic acid with appropriate phenols, followed by acetylation in 50-83% overall yields. All hydroxy- and acetoxycoumarins were unambiguously identified on the basis of their spectral data. Candida antarctica lipase-catalysed deacetylation of these racemic acetoxydihydrocoumarins in dioxane occurred with moderate enantioselectivity. This is one of the rare examples of resolution using phenolic ester moiety as a remote handle for chiral recognition by a lipase.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Candida / enzymology
  • Catalysis
  • Chromatography, Thin Layer
  • Coumarins / chemical synthesis*
  • Coumarins / chemistry
  • Dealkylation
  • Dioxanes / chemical synthesis
  • Lipase / metabolism*
  • Magnetic Resonance Spectroscopy
  • Pancrelipase / metabolism
  • Spectrophotometry, Ultraviolet
  • Spectroscopy, Fourier Transform Infrared
  • Stereoisomerism
  • Swine

Substances

  • Coumarins
  • Dioxanes
  • Pancrelipase
  • Lipase