Highly substituted pyrido[4,3‐b]indole derivatives were synthesized through a straightforward one‐pot silver‐catalyzed process involving 2‐alkynylindole‐3‐carbaldehyde oximes. The tandem cyclization/nucleophilic addition sequence was optimized and applied to a wide range of nucleophiles, which reacted regioselectively at the pyrido[4,3‐b]indole C4 position. The scope and limitations of the methodology were evaluated and the final compounds were obtained in fair to very good yields. This versatile method proved to be compatible with various chemical functionalities or (hetero)cycles.

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