Indoles with aromatic substituents at C3 are an important class of compounds. This motif can be found in a large variety of bioactive molecules such as Fluvastatine 1 that targets the HMG-CoA receptor to lower the LDL cholesterol and compound 2 which was identified as a potential treatment against the uterine fibroid and targets progesterone receptors (Figure 1a). Aromatic groups are commonly installed at C3 position of indoles via by metal-catalyzed cross coupling reactions, C–H activation processes or via metal-free transformation using hypervalent iodine reagents. Herein, we report our results on the C3-arylation of indoles using pentavalent organobismuth compounds. The reaction, which is based on the work of Barton,5 uses catalytic amounts of copper(II) trifluoroacetate, operates under simple conditions and shows excellent substrate and bismuth scope (Figure 1b).

C3-arylation of indole using organobismuthin reagent

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