Dynamic kinetic resolution based asymmetric transfer hydrogenation of α-alkoxy-β-ketophosphonates. Diastereo- and enantioselective synthesis of monoprotected 1,2-dihydroxyphosphonates

J Org Chem. 2014 Mar 21;79(6):2666-81. doi: 10.1021/jo500148j. Epub 2014 Mar 6.

Abstract

Dynamic kinetic resolution driven, asymmetric transfer hydrogenation reactions of a wide range of 2-substituted α-alkoxy-β-ketophosphonates 3 were observed to proceed efficiently to give the corresponding 2-substituted α-alkoxy-β-hydroxy phosphonates 4 with excellent levels of diastereo- and enantioselectivity. These processes are promoted by using well-defined, commercially available, chiral transition metal catalysts and a 0.2:1 mixture of formic acid and triethylamine as the hydrogen source and solvent.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalysis
  • Ethylamines / chemistry*
  • Formates / chemistry*
  • Hydrogenation
  • Ketones / chemistry*
  • Kinetics
  • Molecular Structure
  • Organophosphonates / chemical synthesis*
  • Organophosphonates / chemistry
  • Stereoisomerism
  • Transition Elements / chemistry*

Substances

  • Ethylamines
  • Formates
  • Ketones
  • Organophosphonates
  • Transition Elements
  • triethylamine