Synthesis of Substituted 4-(1H-indol-6-yl)-1H-indazoles as Potential PDK1 Inhibitors

Document Type


Publication Date


Publication Details

This article was originally published as:

Brzozowski, M., O'Brien, N. J., Wilson, D. J., & Abbott, B. M. (2014). Synthesis of substituted 4-(1H-indol-6-yl)-1H-indazoles as potential PDK1 inhibitors. Tetrahedron, 70(2), 318-326. doi:10.1016/j.tet.2013.11.054



The development of a preparative route to a series of novel 4-(1H-indol-6-yl)-1H-indazole compounds as potential PDK1 inhibitors is described. The synthetic strategy centres on the late-stage Suzuki crosscoupling of N-unprotected indazole and indole fragments. The use of a monoligated palladium catalyst system was found to be highly beneficial in the cross-coupling reaction. The indazole and indole fragments were constructed by diazotisation/cyclisation and SNAr/reductive cyclisation sequences, respectively.


Due to copyright restrictions this article is unavailable for download.

This article may be accessed from the publisher here.

At the time of writing David Wilson was affiliated with Avondale College as a Conjoint Lecturer.