Trideuteromethylation Enabled by a Sulfoxonium Metathesis Reaction

Org Lett. 2019 Jan 18;21(2):448-452. doi: 10.1021/acs.orglett.8b03641. Epub 2019 Jan 7.

Abstract

A conceptually novel sulfoxonium metathesis reaction between TMSOI and cost-effective DMSO- d6 is developed for the efficient generation of a new trideuteromethylation reagent TDMSOI. The new reagent TDMSOI is produced highly efficiently by simply heating a mixture of TMSOI and DMSO- d6 and directly used for subsequent trideuteromethylation in a "one-pot" operation. The preparative power of the new versatile reagent and the "one-pot" protocol is demonstrated by its use to install the -CD3 moiety into broad functionalities including phenols, thiophenols, acidic amines, and enolizable methylene units in high yield and at a useful level of deuteration (>87% D).

Publication types

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

MeSH terms

  • Deuterium / chemistry*
  • Indicators and Reagents / chemistry*
  • Phenols / chemistry*
  • Sulfhydryl Compounds / chemistry*

Substances

  • Indicators and Reagents
  • Phenols
  • Sulfhydryl Compounds
  • thiophenol
  • Deuterium