<abstract abstract-type="main" xml:lang="en"> <title>Abstract</title> <p>A regioselective microwave‐assisted one‐pot two‐step transformation of 1, 6‐naphthyridin‐2(1H)‐ones consisting of a Buchwald—Hartwig cross‐coupling in position 3 in the first step and a second Buchwald—Hartwig coupling, a Suzuki coupling, or a S<sub>N</sub>Ar reaction in the second step is elaborated.</p> </abstract>