吲哚-2-亚胺与α-芳基乙烯磺酸盐序贯[1 + 2]环化反应合成螺[环丙烷-1,3'-吲哚]-2'-亚胺

IF 2.7 3区 化学 Q1 CHEMISTRY, ORGANIC
Yan Gou , Shanling Hou , Qingyi Fu , Zhi Fan , Yuming Li
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引用次数: 0

摘要

首次实现了吲哚-2-亚胺与α-芳基乙烯磺酸盐的连续[1 + 2]环化反应,得到了一系列功能化螺[环丙烷-1,3'-吲哚]-2'-亚胺,收率为51-95%,具有较高的化学选择性和非对映选择性。该方法操作简单,操作条件温和,底物范围广,官能团容忍度好。此外,一些选定的螺环产物对A549细胞系表现出有希望的抗癌活性,突出了它们在药物筛选中的应用潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Diastereoselective synthesis of spiro[cyclopropane-1,3′-indolin]-2′-imines via a sequential [1 + 2] annulation reaction of indolin-2-imines with α-aryl vinylsulfonium salts†

Diastereoselective synthesis of spiro[cyclopropane-1,3′-indolin]-2′-imines via a sequential [1 + 2] annulation reaction of indolin-2-imines with α-aryl vinylsulfonium salts†
A sequential [1 + 2] annulation reaction of indolin-2-imines with α-aryl vinylsulfonium salts has been achieved for the first time, leading to a series of functionalized spiro[cyclopropane-1,3′-indolin]-2′-imines in 51–95% yields with high chemoselectivity and diastereoselectivity. The method is easy to manipulate, operates under mild conditions, and shows wide substrate scope with good functional group tolerance. Moreover, some of the selected spiro-annulated products exhibit promising anticancer activity against the A549 cell line, highlighting their potential for application in drug screening.
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来源期刊
Organic & Biomolecular Chemistry
Organic & Biomolecular Chemistry 化学-有机化学
CiteScore
5.50
自引率
9.40%
发文量
1056
审稿时长
1.3 months
期刊介绍: Organic & Biomolecular Chemistry is an international journal using integrated research in chemistry-organic chemistry. Founded in 2003 by the Royal Society of Chemistry, the journal is published in Semimonthly issues and has been indexed by SCIE, a leading international database. The journal focuses on the key research and cutting-edge progress in the field of chemistry-organic chemistry, publishes and reports the research results in this field in a timely manner, and is committed to becoming a window and platform for rapid academic exchanges among peers in this field. The journal's impact factor in 2023 is 2.9, and its CiteScore is 5.5.
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