Synthesis 2015; 47(24): 3983-3989
DOI: 10.1055/s-0035-1560089
paper
© Georg Thieme Verlag Stuttgart · New York

Domino 6-endo-dig Cyclization/Halogenation Reactions: Three-Component Synthesis of 1,3-Disubstituted 4-Haloimidazo[1,2-a:4,5-c′]dipyridines

Cécile Enguehard-Gueiffier*
a   UMR INSERM 1069 Nutrition, Croissance et Cancer, Université François Rabelais, 31 avenue Monge, 37200 Tours, France
,
Pierre-Olivier Delaye
b   UMR INRA 1282 Infectiologie et Santé Publique, Recherche et Innovation en Chimie Médicinale, Université François Rabelais, 31 avenue Monge, 37200 Tours, France   Email: cecile.enguehard-gueiffier@univ-tours.fr
,
Mélanie Pénichon
b   UMR INRA 1282 Infectiologie et Santé Publique, Recherche et Innovation en Chimie Médicinale, Université François Rabelais, 31 avenue Monge, 37200 Tours, France   Email: cecile.enguehard-gueiffier@univ-tours.fr
,
Caroline Denevault-Sabourin
b   UMR INRA 1282 Infectiologie et Santé Publique, Recherche et Innovation en Chimie Médicinale, Université François Rabelais, 31 avenue Monge, 37200 Tours, France   Email: cecile.enguehard-gueiffier@univ-tours.fr
,
Hassan Allouchi
b   UMR INRA 1282 Infectiologie et Santé Publique, Recherche et Innovation en Chimie Médicinale, Université François Rabelais, 31 avenue Monge, 37200 Tours, France   Email: cecile.enguehard-gueiffier@univ-tours.fr
,
Alain Gueiffier
a   UMR INSERM 1069 Nutrition, Croissance et Cancer, Université François Rabelais, 31 avenue Monge, 37200 Tours, France
› Author Affiliations
Further Information

Publication History

Received: 22 May 2015

Accepted after revision: 11 July 2015

Publication Date:
11 September 2015 (online)


Abstract

A regiocontrolled 6-endo-dig cyclization of 3-ethynylimidazo[1,2-a]pyridine-2-carbonitriles promoted by Grignard reagent in the presence of iodine has been developed. We optimized the reaction conditions to allow the straightforward synthesis of 1,3-disubstituted 4-iodoimidazo[1,2-a:4,5-c′]dipyridines. Finally, the reactivity of the 4-iodo position toward various metal-catalyzed coupling reactions (Suzuki–Miyaura­, Sonogashira, etc.) or cyanation was successfully evaluated.

Supporting Information

 
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