Enantioselective carbolithiation of S-alkenyl-N-aryl thiocarbamates: kinetic and thermodynamic control

Org Biomol Chem. 2015 Feb 28;13(8):2330-40. doi: 10.1039/c4ob02329c.

Abstract

The addition of n-butyllithium to alkenylthiocarbamates in the presence of (-)-sparteine or the (+)-sparteine surrogate leads to asymmetric carbolithiation, and returns enantiomerically enriched thiocarbamate derivatives of secondary thiols. In THF, with the (+)-sparteine surrogate, in situ aryl migration leads to an enantiomerically enriched tertiary thiol derivative. Remarkably, the two pseudoenantiomeric chiral ligands do not always give enantiomeric products, probably as a result of a complex interplay of kinetic and thermodynamic control. In situ IR and NMR studies of a stable, hindered lithiated thiocarbamate demonstrated its chemical and configurational stability over a period of hours at 0 °C.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Kinetics
  • Magnetic Resonance Spectroscopy
  • Molecular Structure
  • Organometallic Compounds / chemistry
  • Sparteine / chemistry
  • Stereoisomerism
  • Sulfhydryl Compounds / chemical synthesis*
  • Sulfhydryl Compounds / chemistry
  • Thermodynamics*
  • Thiocarbamates / chemistry*

Substances

  • Organometallic Compounds
  • Sulfhydryl Compounds
  • Thiocarbamates
  • butyllithium
  • Sparteine