Ruthenium-Catalyzed Cross Dehydrogenative Annulation of N-(7-Azaindole)benzamides with Maleimides: One-Step Access to Highly Functionalized Pyrroloisoquinoline

A ruthenium(II)-catalyzed cross dehydrogenative annulation of N-(7-azaindole)benzamides with maleimides has been demonstrated. Herein, we have explored the use of N-amino-7-azaindole as a new bidentate directing group for dehydrogenative [4 + 2] annulation. This method works efficiently, affording a variety of pharmacologically useful 7-azaindole-based isoquinolones and showing a wide functional group tolerance.