The C–H arylation of indoles holds the promise to shorten synthetic routes in the production of pharmaceuticals. However, late-stage C–H activation reactions often rely on the presence of protecting groups or stoichiometric metal additives. The regiospecific C–H arylation of a highly functionalized azepino[5,3,4-cd]indole scaffold lacking directing groups via Pd(II) and Cu(II) co-catalysis is reported. The direct C–H coupling was demonstrated in the convergent synthesis of rucaparib, an FDA approved anticancer drug.

中文翻译：

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通过 Pd/Cu 催化氮杂吲哚的后期 C-H 芳基化：Rucaparib 的一步高效和收敛合成

吲哚的 C-H 芳基化有望缩短药物生产中的合成路线。然而，后期 C-H 活化反应通常依赖于保护基团或化学计量金属添加剂的存在。据报道，高度官能化的氮杂[5,3,4- cd ]吲哚支架通过Pd（II）和Cu（II）共催化进行区域特异性C-H芳基化，该支架缺乏导向基团。直接 C-H 偶联在 FDA 批准的抗癌药物 rucaparib 的收敛合成中得到证明。