Synthesis And Antibacterial Studies Of 2-substituted Indoles And Spiropyrrolidine Oxindoles

In this paper,a series of 2-substituted indoles have been synthesized by palladium-catalyzed Suzuki coupling,novel spiropyrrolidine oxindoles have been synthesised via 1,3-diploar cycloaddition and their antibacterial activity have been studied.It consists of the following three parts:Part 1:A new synthetic method for 2-substituted indoles has been developed,the process through Suzuki coupling reaction of 3-bromoindoles with hindered boronic acid catalyzed by Pd（OAc）₂/PCy₃,and a series of 2-substituted indoles have been synthesized in moderate to high yields（65%-96%）.Part 2:Synthesis of novel spiropyrrolidine oxoindoles via Ag-catalyzed[3+2]cycloaddition of azomethine ylides generated in situ from the condensation of substituted isatins and primaryα-amino acid esters with chalcones.The products were smoothly acquired in moderate to high yileds（50-95%）with good to excellent diastereoselectivity（11:1->20:1）.Part 3:Antibacterial activities of the novel Spiropyrrolidine Oxindoles were studied,the bacteria were Staphylococcus aureus、Escherichia coli、Pseudomonas aeruginosa and Bacillus subtilis.Preliminary results showed that the compounds 7r and 9g had good antibacterial activity.