Synthesis of 3-(hetero)aryl tetrahydropyrazolo[3,4-c]pyridines by Suzuki-Miyaura cross-coupling methodology

J Org Chem. 2014 Aug 15;79(16):7682-8. doi: 10.1021/jo5012015. Epub 2014 Jul 29.

Abstract

A new synthetic route to 3-(heteroaryl) tetrahydropyrazolo[3,4-c]pyridines has been developed that uses the Suzuki-Miyaura cross-coupling of a triflate 6 with (hetero)aryl boronic acids or esters. Using Pd(OAc)2 and XPhos or an XPhos precatalyst, a diverse range of substituents at the C3 position of the tetrahydropyrazolo[3,4-c]pyridine skeleton were prepared. The use of pivaloyloxymethyl and benzyl protection also offers the potential to differentially functionalize the pyrazole and tetrahydropyridine nitrogens.

MeSH terms

  • Benzyl Compounds / chemistry*
  • Catalysis
  • Esters
  • Molecular Structure
  • Palladium / chemistry*
  • Pyrazoles / chemical synthesis*
  • Pyrazoles / chemistry*
  • Pyridines / chemical synthesis*
  • Pyridines / chemistry*

Substances

  • Benzyl Compounds
  • Esters
  • Pyrazoles
  • Pyridines
  • Palladium