Nickel/NHC‐Catalyzed Enantioselective Cyclization of Pyridones and Pyrimidones with Tethered Alkenes,Advanced Synthesis & Catalysis

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Nickel/NHC‐Catalyzed Enantioselective Cyclization of Pyridones and Pyrimidones with Tethered Alkenes
Advanced Synthesis & Catalysis ( IF 4.4 ) Pub Date : 2020-01-22 , DOI: 10.1002/adsc.201901582
Di Shen _{1,

2} , Wu‐Bin Zhang ₂ , Zhiyang Li ₂ , Shi‐Liang Shi ₂ , Youjun Xu ₁

Affiliation

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.

中文翻译：

镍/ NHC催化的吡啶酮和嘧啶与链状烯烃的对映选择性环化

报道了2-和4-吡啶酮和4-嘧啶酮与烯烃的高度对映选择性Ni（0）催化的内选择性CH环化反应，可提供与药物相关的双环杂环产物。使用易于制备的手性庞大的NHC配体（SIPE）作为Ni催化剂和市售的AlEt ₃作为助催化剂，可以提高该反应的实用性。

更新日期：2020-01-23

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