Rapid access to C2-quaternary 3-methyleneindolines via base-mediated post-Ugi Conia-ene cyclization
Shuang Zhao1, Yi He1, Feiyu Gao1
1Center for Novel Target and Therapeutic Intervention, Institute of Life Sciences, Chongqing Medical University, Chongqing 400016, China. heyisky@cqmu.edu.cn.
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.
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