Comprehensive SummaryHerein, we present a facile synthesis of amide‐type water‐soluble fullerene derivatives decorated with five residues of amino acids. As compared to the previously developed approaches, the proposed method enables usage of a broad range of amino acids, including those unstable under Friedel‐Crafts reaction conditions. Furthermore, it is fully tolerant to the nature of the sixth addend X in C₆₀R₅X precursor compounds and allows one to obtain fullerene derivatives with X=Cl, H, alkyl. The synthesized amide‐type water‐soluble fullerene derivatives demonstrated promising antiviral activities against rimantadine‐resistant influenza А/Puerto Rico/8/34 (Н1N1) virus in vitro.