Efficient synthesis of beta-hydroxy-alpha-amino acid derivatives via direct catalytic asymmetric aldol reaction of alpha-isothiocyanato imide with aldehydes

Chemistry. 2010 Sep 3;16(33):10124-9. doi: 10.1002/chem.201000284.

Abstract

An easily available and efficient chiral N,N'-dioxide-nickel(II) complex catalyst has been developed for the direct catalytic asymmetric aldol reaction of alpha-isothiocyanato imide with aldehydes which produces the products in morderate to high yields (up to 98 %) with excellent diastereo- (up to >99:1 d.r.) and enantioselectivities (up to >99 % ee). A variety of aromatic, heteroaromatic, alpha,beta-unsaturated, and aliphatic aldehydes were found to be suitable substrates in the presence of 2.5 mol % L-proline-derived N,N'-dioxide L5-nickel(II) complex. This process was air-tolerant and easily manipulated with available reagents. Based on experimental investigations, a possible transition state has been proposed to explain the origin of reactivity and asymmetric inductivity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aldehydes / chemistry*
  • Amino Acids / chemical synthesis*
  • Amino Acids / chemistry
  • Catalysis
  • Imides / chemistry*
  • Isothiocyanates / chemistry*
  • Nickel / chemistry
  • Nitrogen Oxides / chemistry
  • Organometallic Compounds / chemistry
  • Stereoisomerism

Substances

  • Aldehydes
  • Amino Acids
  • Imides
  • Isothiocyanates
  • Nitrogen Oxides
  • Organometallic Compounds
  • Nickel