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

Publication Date
2014-01-14
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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.

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Keywords
3-Phosphoinositide-dependent kinase 1 (PDK1), 4-(1H-Indol-6-yl)-1H-indazole, Inhibitor, Suzuki cross-coupling
Citation

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

International Standard Serial Number
0040-4020
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