An efficient route to chiral N-heterocycles bearing a C-F stereogenic center via asymmetric hydrogenation of fluorinated isoquinolines

Chem Commun (Camb). 2013 Oct 4;49(76):8537-9. doi: 10.1039/c3cc45341c.

Abstract

An efficient iridium-catalyzed asymmetric hydrogenation of the fluorinated isoquinoline derivatives has been successfully developed for the synthesis of chiral fluorinated tetrahydroisoquinoline derivatives with up to 93% ee. This methodology features the use of a hydrochloride salt as well as a catalytic amount of halogenated hydantoin which were vital for the reactivity, enantioselectivity, and inhibition of the hydrodefluorination pathway.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalysis
  • Heterocyclic Compounds / chemistry*
  • Hydrocarbons, Fluorinated / chemical synthesis*
  • Hydrocarbons, Fluorinated / chemistry
  • Hydrogenation
  • Iridium / chemistry
  • Isoquinolines / chemistry*
  • Molecular Structure
  • Stereoisomerism

Substances

  • Heterocyclic Compounds
  • Hydrocarbons, Fluorinated
  • Isoquinolines
  • Iridium