N-Arylation of Amino Acid Esters via an I2-Mediated Metal-Free Multicomponent Benzannulation Strategy

文献类型: 外文期刊

第一作者: Shi, Liqiao

作者: Shi, Liqiao;Wu, Hongqu;Ke, Shaoyong;Huang, Wenbo;Yang, Bing;Kuang, Buxiao;Rao, Xiaofeng;Rao, Xiaofeng;Liu, Changhui

作者机构:

期刊名称:JOURNAL OF ORGANIC CHEMISTRY ( 影响因子:3.6; 五年影响因子:3.4 )

ISSN: 0022-3263

年卷期: 2023 年 88 卷 23 期

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收录情况: SCI

摘要: Herein, we present a novel method for the N-arylation of amino acid esters using alpha-bromoacetaldehyde acetal and acetoacetate via an I2-mediated metal-free benzannulation strategy, which disclosed the first synthetic application of N-arylation of amino acids using nonaromatic building blocks. The synthesized N-arylated amino acid derivatives were found to possess promising selective inhibition against human hepatocellular liver carcinoma cells, human melanoma cells, and human normal liver cells, with an IC50 value as low as 16.79 mu g center dot( -1).

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