Stereocontrolled fluorobenzylation of vinyl sulfones and α,β-unsaturated esters mediated by a remote sulfinyl group. Synthesis of functionalized enantiomerically pure benzylic fluorides

J Org Chem. 2012 Mar 16;77(6):2893-900. doi: 10.1021/jo300174k. Epub 2012 Mar 6.

Abstract

A sulfinyl group in an ortho position confers enough chemical and configurational stability to monofluorobenzylcarbanions to evolve in a completely stereoselective way in their reactions with β-substituted vinyl sulfones and α,β-unsaturated esters. Reactions afford easily separable mixtures of two epimers differing in the configuration of the center derived from the Michael acceptor (up to 98% de). They can be easily converted into enantiomerically pure γ-fluorinated γ-phenylsulfones and γ-phenylesters bearing two chiral centers.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Esters
  • Fluorides / chemistry*
  • Hydrocarbons, Fluorinated / chemical synthesis*
  • Hydrocarbons, Fluorinated / chemistry*
  • Molecular Structure
  • Stereoisomerism
  • Sulfones / chemistry*

Substances

  • Esters
  • Hydrocarbons, Fluorinated
  • Sulfones
  • divinyl sulfone
  • Fluorides