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