Remdesivir was the first emergence treatment for COVID-19 allowed by Anvisa. Our research group has described improvements of Klein’s route for obtaining Remdesivir’s nucleobase in 3 steps and 39% overall yield (Scheme 1).1 In this present work, after the amine protection step,2 we developed a methodology that allows the regioselective iodination of this nucleobase through a C-H activation promoted by the Knochel-Hauser base TMPMgCl.LiCl. The developed process consists of an initial magnesiation step followed by the electrophile (I2) attack. During our studies, the temperature, was evaluated and 0 °C showed to be the best (Table 1- entries 1 and 2). In addition, an excess of TMPMgCl.LiCl and iodine (4 equiv.) were important to improve the formation of the product (Table 1- entry 4). In conclusion, the iodide nucleobase was synthesized in 15% overall yield in mild reaction conditions via C-H activation. For future works, we desire to evaluate the glycosylation step using this advanced intermediate.