Oxyamination of Unactivated Alkenes with Electron-Rich Amines and Acids via a Catalytic Triiodide Intermediate

Org Lett. 2020 Feb 7;22(3):884-890. doi: 10.1021/acs.orglett.9b04432. Epub 2020 Jan 13.

Abstract

An aerobic catalytic oxidation process is described for the olefin oxyamination using acids and primary amines as the sources of O and N. Our mechanistic findings point to the formation of triiodide as a critical catalytic intermediate to account for the tolerance of electron-rich nucleophiles. This dual iodide and copper catalytic system is suitable for a formal [5+1] annulation process to access valuable lactam structures and highlighted by the synthesis of the pharmaceutical Zamifenacin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkenes / chemistry*
  • Amination
  • Amines / chemistry*
  • Carboxylic Acids / chemistry*
  • Catalysis
  • Copper / chemistry
  • Dioxoles / chemical synthesis*
  • Dioxoles / chemistry
  • Electrons*
  • Iodides / chemistry*
  • Molecular Structure
  • Oxidation-Reduction
  • Piperidines / chemical synthesis*
  • Piperidines / chemistry
  • Stereoisomerism

Substances

  • Alkenes
  • Amines
  • Carboxylic Acids
  • Dioxoles
  • Iodides
  • Piperidines
  • Copper
  • zamifenacin