N-Arylation of Amino Acid Esters via an I2-Mediated Metal-Free Multicomponent Benzannulation Strategy
文献类型： 外文期刊
作者： Huang, Wenbo 2 ; Rao, Xiaofeng 3 ; Shi, Liqiao 1 ; Yang, Bing 2 ; Kuang, Buxiao 2 ; Wu, Hongqu 1 ; Ke, Shaoyong 1 ; Liu, Changhui 5 ;
作者机构： 1.Hubei Acad Agr Sci, Minist Agr & Rural Affairs, Hubei Biopesticide Engn Res Ctr, Key Lab Microbial Pesticides, Wuhan 430064, Peoples R China
2.Hubei Three Gorges Lab, Yichang 443007, Peoples R China
3.Southern Univ Sci & Technol, Shenzhen Grubbs Inst, Shenzhen 518055, Peoples R China
4.Shenzhen Bay Lab, Shenzhen 518055, Peoples R China
5.China Univ Min & Technol, Sch Low Carbon Energy & Power Engn, Xuzhou 221116, Peoples R China
期刊名称：JOURNAL OF ORGANIC CHEMISTRY （ 2022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
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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