Litcius/Paper detail

Divergent Synthesis of Pyrazolo[1,5-<i>a</i>]pyridines and Imidazo[1,5-<i>a</i>]pyridines via Reagent-Controlled Cleavage of the C–N or C–C Azirine Bond in 2-Pyridylazirines

Anastasiya V. Agafonova, Artem A. Golubev, Ilia A. Smetanin, Alexander F. Khlebnikov, Dar’ya V. Spiridonova, Михаил С. Новиков

2023Organic Letters15 citationsDOI

Abstract

The three-membered ring in 2-(2-pyridyl)azirine-2-carboxylic esters and thioesters can undergo selective cleavage of either the N–C2 bond under copper(II) catalysis or the C–C bond under the action of HCl to provide isomeric azirine ring expansion products of pyrazolo[1,5- a ]pyridine or imidazo[1,5- a ]pyridine series, respectively. Mild catalytic reaction conditions for the formation of pyrazolopyridines make it possible to obtain them directly from 4-bromoisoxazoles by a one-pot, three-stage procedure without isolating the intermediate 2-bromoazirines and 2-(2-pyridyl)azirines.

Topics & Concepts

AzirineChemistryReagentPyridineCleavage (geology)Ring (chemistry)CatalysisBond cleavageMedicinal chemistryStereochemistryOrganic chemistryEngineeringFracture (geology)Geotechnical engineeringSynthesis and Catalytic ReactionsCatalytic C–H Functionalization MethodsPhenothiazines and Benzothiazines Synthesis and Activities