A cobalt-catalyzed annulation of the C(sp²)–H/N–H bond of indoloamides with alkynes assisted by 8-aminoquinoline is reported for the synthesis of six-membered indololactams. The use of salicylaldehyde as the ligand is crucial for this transformation. The protocol has a broad scope for both alkynes and indoles. Preparing an active Co complex illustrates that salicylaldehyde plays a key role in the C–H activation step. The synthetic applications are proven by the gram-scale reaction and one-step construction of the multicyclic 5-HT3 receptor antagonist.

中文翻译：

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水杨醛促进钴催化 C-H/N-H 环化吲哚酰胺与炔烃：直接合成 5-HT3 受体拮抗剂类似物

据报道，在 8-氨基喹啉的辅助下，吲哚酰胺的 C(sp ² )-H/N-H 键与炔烃的钴催化环化可用于合成六元吲哚内酰胺。使用水杨醛作为配体对于这种转化至关重要。该协议对炔烃和吲哚都有广泛的适用范围。制备活性 Co 复合物说明水杨醛在 C-H 活化步骤中起关键作用。合成应用通过多环 5-HT3 受体拮抗剂的克级反应和一步构建得到证实。