Synthesis of novel tetrahydro-1H-pyrazolo[4,3-c]pyridines via intramolecular nitrilimine cycloaddition

Chem Pharm Bull (Tokyo). 2012;60(8):1063-6. doi: 10.1248/cpb.c110498.

Abstract

The preparation of novel tetrahydro-1H-pyrazolo[4,3-c]pyridines is reported. Pivotal to the synthesis of these compounds was the development of mild reaction conditions to generate a highly functionalized nitrilimine capable of undergoing an intramolecular cycloaddition with a tethered alkyne. The desired cycloadduct was formed as an equal mixture of diastereomers.

MeSH terms

  • Cyclization*
  • Imines / chemistry*
  • Magnetic Resonance Spectroscopy
  • Mass Spectrometry
  • Models, Molecular
  • Nitriles / chemistry*
  • Pyridines / chemical synthesis*

Substances

  • Imines
  • Nitriles
  • Pyridines