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Synthesis of Imidazo[1,2-<i>a</i>]pyridines via Near UV Light-Induced Cyclization of Azirinylpyridinium Salts

Ilya P. Filippov, Anastasiya V. Agafonova, Gleb D. Titov, Ilia A. Smetanin, Николай В. Ростовский, Alexander F. Khlebnikov, Михаил С. Новиков

2022The Journal of Organic Chemistry26 citationsDOI

Abstract

An efficient one-pot synthesis of imidazo[1,2-a]pyridines from 2-bromoazirines and pyridines has been developed. The construction of the bicyclic framework of imidazo[1,2-a]pyridines occurs in two steps through the formation of (2H-azirin-2-yl)pyridinium bromides followed by dehydrobrominative UV light-induced cyclization. The method can also be applied for the synthesis of imidazo[2,1-a]isoquinolines. Unstable in solution, (2H-azirin-2-yl)pyridinium/isoquinolinium bromides were quantitatively converted to stable tetrafluoroborates, which can be cyclized to imidazo[1,2-a]pyridines under UV irradiation in the presence of bromide ions.

Topics & Concepts

ChemistryPyridiniumBicyclic moleculeBromideMedicinal chemistryIonCombinatorial chemistryPyridinium CompoundsOrganic chemistryCatalytic C–H Functionalization MethodsSynthesis and Catalytic ReactionsPhenothiazines and Benzothiazines Synthesis and Activities
Synthesis of Imidazo[1,2-<i>a</i>]pyridines via Near UV Light-Induced Cyclization of Azirinylpyridinium Salts | Litcius