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Cs(2)CO(3) catalyzed direct aza-Michael addition of azoles to α,β-unsaturated malonates

A highly efficient method for the synthesis of azole derivatives via a direct aza-Michael addition of azoles to α,β-unsaturated malonates using Cs(2)CO(3) as a catalyst, has been successfully developed. A series of azole derivatives have been obtained in up to 94% yield and the reaction could be amp...

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Detalles Bibliográficos
Autores principales: Jiang, Zi-Yu, Huang, Zhe-Yao, Yang, Hong, Zhou, Lin, Li, Qing-Han, Zhao, Zhi-Gang
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9248005/
https://www.ncbi.nlm.nih.gov/pubmed/35865588
http://dx.doi.org/10.1039/d2ra02314h
Descripción
Sumario:A highly efficient method for the synthesis of azole derivatives via a direct aza-Michael addition of azoles to α,β-unsaturated malonates using Cs(2)CO(3) as a catalyst, has been successfully developed. A series of azole derivatives have been obtained in up to 94% yield and the reaction could be amplified to gram scale in excellent yield in the presence of 10 mol% of Cs(2)CO(3).