当前位置: X-MOL 学术Synlett › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
A [4+3] Cycloaddition Reaction of Aza-ortho-quinone Methides with C,N-Cyclic Azomethine Imines for Synthesis of 1,2,4-Triazepines
Synlett ( IF 1.7 ) Pub Date : 2021-08-12 , DOI: 10.1055/a-1585-4490
Yunlei Hou , Ping Gong , Xinyue Wang , Zefei Li , Chang Feng , Qi Zhen , Mingzhang Guo , Yaning Yao , Xinyu Zou , Pengfei Wang

The base-induced formal [4+3] cycloaddition reaction of C,N-cyclic azomethine imines with aza-ortho-quinone methides, generated in situ, is reported. This protocol provided an efficient method for the synthesis of biologically important 1,2,4-triazepine derivatives, with a wide substrate scope and excellent functional-group tolerance, and it gives moderate to excellent yields under mild conditions. Several of the derivatives exhibited in vitro antitumor activities against the A2780 cell line in a screening of the cancer cell lines HCT-116, H2228, and A2780 by an MTT assay.

中文翻译:

Aza-ortho-quinone Methides 与 C,​​N-Cyclic Azomethine 亚胺的 [4+3] 环加成反应合成 1,2,4-三氮杂

报告了碱诱导的正式 [4+3] 环加成反应,C,N-环状偶氮甲亚胺与氮杂邻醌甲基化物,原位生成。该协议为合成具有生物学意义的 1,2,4-三氮杂衍生物提供了一种有效的方法,具有广泛的底物范围和优异的官能团耐受性,并且在温和条件下可提供中等至优异的产率。在通过 MTT 分析筛选癌细胞系 HCT-116、H2228 和 A2780 时,几种衍生物表现出对 A2780 细胞系的体外抗肿瘤活性。
更新日期:2021-08-25
down
wechat
bug