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铜介导的芳基乙酸和 1,3-二羰基化合物的脱羧偶联反应。

Copper-Mediated Decarboxylative Coupling between Arylacetic Acids and 1,3-Dicarbonyl Compounds.

机构信息

Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, 1023 South Shatai Road, Baiyun District, Guangzhou 510515, PR China.

出版信息

Org Lett. 2021 Oct 15;23(20):7878-7882. doi: 10.1021/acs.orglett.1c02897. Epub 2021 Oct 6.

Abstract

A copper-mediated decarboxylative coupling reaction between arylacetic acids and 1,3-dicarbonyl compounds was described. Significantly, methanocycloocta[]indoles were also obtained by sequential intramolecular dehydrocyclization process in some cases. This protocol featured a broad substrate scope, simple operations, and good yields. Moreover, the products exhibited potent antiproliferative activity against the human cancer cell lines by a MTT assay.

摘要

本文描述了一种铜介导的芳基乙酸和 1,3-二羰基化合物的脱羧偶联反应。在某些情况下,通过顺序的分子内环脱氢环化过程,还可以得到甲硫环[8]吲哚类化合物。该方法具有广泛的底物范围、操作简单和产率高等特点。此外,通过 MTT 测定法,这些产物对人癌细胞系表现出很强的抗增殖活性。

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