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 cross-coupling 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 S_NAr/reductive cyclisation sequences, respectively.

中文翻译：

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取代的4-（1 H-吲哚-6-基）-1 H-吲唑类化合物作为潜在的PDK1抑制剂的合成

描述了制备一系列潜在的PDK1抑制剂的新型4-（1 H-吲哚-6-基）-1 H-吲唑化合物的制备方法。合成策略集中在未保护的N-吲唑和吲哚片段的Suzuki晚期偶联反应上。发现单连接的钯催化剂体系在交叉偶联反应中是非常有益的。吲唑和吲哚片段通过重氮化/环化和S构成_Ñ分别的Ar /还原环化的序列。