Expedient synthesis of α-heteroaryl piperidines using a Pd-catalyzed Suzuki cross-coupling-reduction sequence

Org Lett. 2014 Jan 17;16(2):413-5. doi: 10.1021/ol403367b. Epub 2014 Jan 3.

Abstract

A method for the modular synthesis of α-heteroaryl piperidines is reported. The two-step procedure consists of an initial Pd-catalyzed Suzuki cross-coupling of the heteroaryl bromide with a boronate ester derived from N-Boc piperidone, followed by subsequent tetrahydropyridine reduction. Using this method, α-heteroaryl piperidine products featuring a broad range of pharmaceutically relevant azine and diazine substitutions have been prepared.

MeSH terms

  • Boronic Acids / chemistry
  • Catalysis
  • Esters
  • Heterocyclic Compounds / chemical synthesis*
  • Heterocyclic Compounds / chemistry
  • Hydrocarbons, Brominated / chemistry*
  • Molecular Structure
  • Palladium / chemistry*
  • Piperidines / chemical synthesis*
  • Piperidines / chemistry

Substances

  • Boronic Acids
  • Esters
  • Heterocyclic Compounds
  • Hydrocarbons, Brominated
  • Piperidines
  • Palladium