Nickel/NHC‐Catalyzed Enantioselective Cyclization of Pyridones and Pyrimidones with Tethered Alkenes

Reported is a highly enantioselective Ni(0)‐catalyzed endo‐selective C−H annulation of 2‐ and 4‐pyridone, and 4‐pyrimidone with alkenes to provide drug‐relevant bicyclic heterocycle products. The use of a readily prepared chiral bulky NHC ligand (SIPE) for Ni catalyst and commercially available AlEt...

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Veröffentlicht in:Advanced synthesis & catalysis 2020-03, Vol.362 (5), p.1125-1130
Hauptverfasser: Shen, Di, Zhang, Wu‐Bin, Li, Zhiyang, Shi, Shi‐Liang, Xu, Youjun
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Sprache:eng
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Zusammenfassung:Reported is a highly enantioselective Ni(0)‐catalyzed endo‐selective C−H annulation of 2‐ and 4‐pyridone, and 4‐pyrimidone with alkenes to provide drug‐relevant bicyclic heterocycle products. The use of a readily prepared chiral bulky NHC ligand (SIPE) for Ni catalyst and commercially available AlEt3 as co‐catalyst enhanced the practicality of this reaction.
ISSN:1615-4150
1615-4169
DOI:10.1002/adsc.201901582