Ruthenium-Catalyzed Regioselective C(sp²)–H Activation/Annulation of <i>N</i>‑(7-Azaindole)amides with 1,3-Diynes Using <i>N</i>‑Amino-7-azaindole as the <i>N</i>,<i>N</i>‑Bidentate Directing Group

The ruthenium­(II)-catalyzed regioselective annulation of N-(7-azaindole)­amides with 1,3-diynes has been demonstrated. Bioactive N-amino-7-azaindole has been used as a new bidentate directing group to furnish an array of 3-alkynylated isoquinolones. Furthermore, the developed protocol works efficiently for both aryl- and heteroaryl-substituted amides producing a range of pharmacologically useful 7-azaindole-based isoquinolones with a wide range of functionality.