Cs2CO3 catalyzed direct aza-Michael addition of azoles to α,β-unsaturated malonates

Zi-Yu Jiang; Zhe-Yao Huang; Hong Yang; Lin Zhou; Qing-Han Li; Zhi-Gang Zhao

doi:10.1039/D2RA02314H

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Cs₂CO₃ catalyzed direct aza-Michael addition of azoles to α,β-unsaturated malonates†

Zi-Yu Jiang,^a Zhe-Yao Huang,^a Hong Yang,^a Lin Zhou,

*^a Qing-Han Li^a and Zhi-Gang Zhao^a

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* Corresponding authors

^a Key Laboratory of General Chemistry of the National Ethnic Affairs Commission, College of Chemistry and Environment, Southwest Minzu University, Chengdu 610041, P. R. China
E-mail: zhoulin@swun.edu.cn

Abstract

A highly efficient method for the synthesis of azole derivatives via a direct aza-Michael addition of azoles to α,β-unsaturated malonates using Cs₂CO₃ 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 Cs₂CO₃.

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Article information

DOI: https://doi.org/10.1039/D2RA02314H
Article type: Paper
Submitted: 10 Apr 2022
Accepted: 27 Jun 2022
First published: 01 Jul 2022
This article is Open Access

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RSC Adv., 2022,12, 19265-19269

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Cs₂CO₃ catalyzed direct aza-Michael addition of azoles to α,β-unsaturated malonates

Z. Jiang, Z. Huang, H. Yang, L. Zhou, Q. Li and Z. Zhao, RSC Adv., 2022, 12, 19265 DOI: 10.1039/D2RA02314H

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