Alkyne Ligation Handles: Propargylation of Hydroxyl, Sulfhydryl, Amino, and Carboxyl Groups via the Nicholas Reaction

Org Lett. 2016 Sep 16;18(18):4566-9. doi: 10.1021/acs.orglett.6b02088. Epub 2016 Aug 29.

Abstract

The Nicholas reaction has been applied to the installation of alkyne ligation handles. Acid-promoted propargylation of hydroxyl, sulfhydryl, amino, and carboxyl groups using dicobalt hexacarbonyl-stabilized propargylium ions is reported. This method is useful for introduction of propargyl groups into base-sensitive molecules, thereby expanding the toolbox of methods for the incorporation of alkynes for bio-orthogonal reactions. High-value molecules are used as the limiting reagent, and various propargylium ion precursors are compared.

Publication types

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

MeSH terms

  • Alkynes / chemistry*
  • Carbon Monoxide / chemistry*
  • Cobalt / chemistry
  • Hydroxyl Radical / chemistry*
  • Molecular Structure
  • Pargyline / analogs & derivatives
  • Pargyline / chemical synthesis*
  • Pargyline / chemistry
  • Proline / analogs & derivatives
  • Proline / chemistry*
  • Sulfhydryl Compounds / chemistry*

Substances

  • Alkynes
  • Sulfhydryl Compounds
  • Hydroxyl Radical
  • Cobalt
  • Carbon Monoxide
  • Proline
  • Pargyline