Highly diastereoselective addition of nitromethane anion to chiral alpha-amidoalkylphenyl sulfones. Synthesis of optically active alpha-amino acid derivatives

Org Biomol Chem. 2003 Dec 7;1(23):4275-81. doi: 10.1039/b309211a. Epub 2003 Oct 23.

Abstract

Optically active syn-alpha-amidoalkylphenyl sulfones can be prepared from chiral aldehydes in anhydrous conditions using benzenesulfinic acid. These sulfones in basic conditions give N-acylimines that react with sodium methanenitronate to afford the corresponding nitro adducts with high anti diastereoselectivity. PM3 semiempirical calculations provide a rationale for the observed opposite stereoselectivity. The obtained nitro derivatives undergo a Nef reaction followed by a methylation giving optically active beta-hydroxy-alpha-amino acid and alpha,beta-diamino acid esters in good yield. These amino acid derivatives are important building blocks for the preparation of biologically active compounds.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aldehydes / chemistry
  • Alkylation
  • Amination
  • Amino Acids / chemical synthesis*
  • Amino Acids / chemistry*
  • Anions / chemistry*
  • Crystallography, X-Ray
  • Methane / analogs & derivatives*
  • Methane / chemistry*
  • Models, Molecular
  • Molecular Conformation
  • Nitroparaffins / chemistry*
  • Stereoisomerism
  • Sulfones / chemistry*
  • Thermodynamics

Substances

  • Aldehydes
  • Amino Acids
  • Anions
  • Nitroparaffins
  • Sulfones
  • Methane
  • nitromethane