One-Pot Reactions for Modular Synthesis of Polysubstituted and Fused Pyridines

A 2-fluoro-1,3-dicarbonyl-initiated one-pot Michael addition/[5 + 1] annulation/dehydrofluorinative aromatization reaction sequence is introduced for regioselective synthesis of di-, tri-, tetra-, and pentasubstituted pyridines as well as fused pyridines. This simple and modular synthesis is perform...

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Bibliographic Details
Published in:Organic letters 2016-11, Vol.18 (21), p.5640-5643
Main Authors: Song, Zhidong, Huang, Xin, Yi, Wenbin, Zhang, Wei
Format: Article
Language:English
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Summary:A 2-fluoro-1,3-dicarbonyl-initiated one-pot Michael addition/[5 + 1] annulation/dehydrofluorinative aromatization reaction sequence is introduced for regioselective synthesis of di-, tri-, tetra-, and pentasubstituted pyridines as well as fused pyridines. This simple and modular synthesis is performed using readily available starting materials and under transition-metal catalyst-free conditions.
ISSN:1523-7060
1523-7052
DOI:10.1021/acs.orglett.6b02883