Thiooxindole is a very important heterocyclic skeleton, which is widely found in natural products and pharmaceutical molecules. In this paper, thiooxindole derivatives were synthesized using diazothiooxindoles and indoles as raw materials under catalysis of rhodium acetate. After optimum reaction conditions were discussed, we found that C3-H bond insertion of indoles were main products with good regioselectivity. The structure of product was confirmed by 1H NMR, 13C NMR, and HRMS. At the same time, activities of products were also tested, including NIH-3T3, B16-F10, 4T1 and HCT116. The results showed that the product exhibited a certain degree of antitumor activity. This reaction system has been proved simple to operate and atom-economic.
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