Title

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

Document Type

Article

Publication Date

1-2014

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

ISSN:0040-4020

ANZSRC / FoR Code

030701 Quantum Chemistry

Abstract

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.

Comments

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