Diastereo- and enantioselective synthesis of (E)-2-Methyl-1,2-syn- and (E)-2-Methyl-1,2-anti-3-pentenediols via allenylboronate kinetic resolution with ((d)Ipc)2BH and aldehyde allylboration

Org Lett. 2012 Jun 15;14(12):3028-31. doi: 10.1021/ol3010968. Epub 2012 May 30.

Abstract

Enantioselective hydroboration of racemic allenylboronate (±)-1 with 0.48 equiv of ((d)Ipc)(2)BH at -25 °C proceeds with efficient kinetic resolution and provides allylborane (R)-Z-4. When heated to 95 °C, allylborane (R)-Z-4 isomerizes to the thermodynamically more stable allylborane isomer (S)-E-7. Subsequent allylboration of aldehydes with (R)-Z-4 or (S)-E-7 at -78 °C followed by oxidative workup provides 1,2-syn- or 1,2-anti-diols, 2 or 3, respectively, in 87-94% ee.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aldehydes / chemistry*
  • Boric Acids / chemistry*
  • Boron Compounds / chemical synthesis*
  • Heterocyclic Compounds, 1-Ring / chemical synthesis*
  • Hydrogenation
  • Kinetics
  • Methylation
  • Molecular Structure
  • Stereoisomerism
  • Thermodynamics

Substances

  • Aldehydes
  • Boric Acids
  • Boron Compounds
  • Heterocyclic Compounds, 1-Ring
  • boric acid