Ruthenium-Catalyzed Regioselective C(sp2)-H Activation/ Annulation of N-(7-Azaindole)amides with 1,3-Diynes Using N-Amino-7-azaindole as the N,N-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.

Automated summary

The study demonstrates the regioselective annulation of N-amino-7-azaindole with 1,3-diynes catalyzed by ruthenium(II). The bioactive N-amino-7-azaindole serves as a new bidentate directing group to produce a range of 3-alkynylated isoquinolones. The protocol is efficient for both aryl- and heteroaryl-substituted amides, resulting in pharmacologically useful 7-azaindole-based isoquinolones with diverse functionalities.