Issue 21, 2023

Rapid access to C2-quaternary 3-methyleneindolines via base-mediated post-Ugi Conia-ene cyclization

Abstract

Highly efficient synthesis of diverse 2,2-disubstituted 3-methyleneindoline derivatives through a one-pot base-promoted post-Ugi 5-exo-dig “Conia-ene”-type cyclization has been disclosed. The mechanism study indicates that an intramolecular hydrogen bond may play a vital role in this process. The antiproliferative evaluation of cancer cell lines reveals that this protocol provides practical use in the green synthesis of bioactive compound libraries.

Graphical abstract: Rapid access to C2-quaternary 3-methyleneindolines via base-mediated post-Ugi Conia-ene cyclization

Supplementary files

Article information

Article type
Communication
Submitted
20 11 2022
Accepted
13 2 2023
First published
14 2 2023

Chem. Commun., 2023,59, 3099-3102

Rapid access to C2-quaternary 3-methyleneindolines via base-mediated post-Ugi Conia-ene cyclization

S. Zhao, Y. He, F. Gao, Y. Wei, J. Zhang, M. Chen, Y. Gao, Y. Zhang, J. Liu, Z. Guo, Z. Li and S. Nie, Chem. Commun., 2023, 59, 3099 DOI: 10.1039/D2CC06281J

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