Stereoselective monofluoromethylation of N-tert-butylsulfinyl ketimines using pregenerated fluoro(phenylsulfonyl)methyl anion

Org Lett. 2008 Dec 4;10(23):5377-80. doi: 10.1021/ol802226k.

Abstract

Pregeneration of fluoro(phenylsulfonyl)methyl anion (PhSO(2)CHF(-)) paves the way for the efficient and highly stereoselective monofluoromethylation of (R)-N-tert-butylsulfinyl ketimines. The stereocontrol mode of the present diastereoselective monofluoromethylation of ketimines is different from the previously known nucleophilic fluoroalkylation of (R)-N-tert-butylsulfinyl aldimines, which suggests that a cyclic six-membered transition state (rather than a nonchelation controlled one) is involved in the current ketimine reaction.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Imines / chemistry*
  • Methylation
  • Nitriles / chemistry*
  • Stereoisomerism
  • Substrate Specificity
  • Sulfonic Acids / chemistry*

Substances

  • Imines
  • Nitriles
  • Sulfonic Acids
  • ketimine