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

Shuang Zhao; Yi He; Feiyu Gao; Yue Wei; Jiawei Zhang; Mengxiao Chen; Yunyun Gao; Yuan Zhang; Jun-Yan Liu; Zufeng Guo; Zhenghua Li; Shenyou Nie

doi:10.1039/D2CC06281J

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

Shuang Zhao,‡^a Yi He,‡*^a Feiyu Gao,‡^a Yue Wei,^a Jiawei Zhang,^a Mengxiao Chen,^a Yunyun Gao,^a Yuan Zhang,^a Jun-Yan Liu,^a Zufeng Guo,^a Zhenghua Li

*^b and Shenyou Nie

*^a

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* Corresponding authors

^a Center for Novel Target and Therapeutic Intervention, Institute of Life Sciences, Chongqing Medical University, Chongqing 400016, China
E-mail: heyisky@cqmu.edu.cn, nieshenyou@cqmu.edu.cn

^b School of Science, Westlake University, Zhejiang 310030, China
E-mail: ahlzhchem@gmail.com

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.

This article is part of the themed collection: ChemComm Milestones – First Independent Articles

Chemical Communications

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

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

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