New enantioselective entry to cycloheptane amino acid polyols

J Org Chem. 2006 Jan 6;71(1):225-30. doi: 10.1021/jo0520137.

Abstract

[reaction: see text] A diversity-oriented protocol has been developed for the assembly of densely hydroxylated cycloheptane amino acids via succession of a vinylogous Mukaiyama aldol reaction (VMAR), a Morita-Baylis-Hillman reaction (MBHR), and an intramolecular pinacol coupling reaction (IPCR). The plan utilizes D- or L-configured glyceraldehyde derivatives as "chiral" surrogates of glyoxal and N-[(tert-butoxycarbonyl)-2-(tert-butyldimethylsilyl)oxy]pyrrole as the synthetic equivalent of the alpha,gamma-dianion of gamma-aminobutanoic acid. The parallel, asymmetric syntheses of four cycloheptane representatives proceed with high diastereocontrol and virtually complete enantioselectivity in ten steps and overall yields of 15-37%.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aldehydes / chemistry
  • Amino Acids / chemistry*
  • Cycloheptanes / chemistry*
  • Magnetic Resonance Spectroscopy
  • Molecular Structure
  • Polymers / chemical synthesis
  • Polymers / chemistry*
  • Stereoisomerism

Substances

  • Aldehydes
  • Amino Acids
  • Cycloheptanes
  • Polymers
  • polyol