| Summary: | Voriconazole (<b>VN</b>) is an antifungal drug indicated for the treatment of several fungal infections. Due to its side effects, some works involving late-stage functionalization of <b>VN</b> have been reported in the literature. Here, we disclose a new <b>VN</b> derivative, the 6-[(2<i>S</i>,3<i>R</i>)-3-(2,4-difluorophenyl)-3-hydroxy-4-(1<i>H</i>-1,2,4-triazol-1-yl)butan-2-yl]-5-fluoropyrimidine-4-carbaldehyde (<b>VN-CHO</b>). This compound results from the photoredox-catalyzed hydroxymethylation of <b>VN</b>, affording a hydroxymethylated derivative (<b>VN-CH<sub>2</sub>OH</b>), followed by oxidation of the former CH<sub>2</sub>OH group. <b>VN-CHO</b> was obtained in good yield (70% yield) and its structure was unveiled by 1D (<sup>1</sup>H and <sup>13</sup>C) and 2D (HSQC and HMBC) NMR techniques. The introduction of a formyl group in <b>VN</b> structure creates a very promising site for further functionalization in a molecule which originally does not have many active sites.
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