Mao-Gui Huang, Shuai Shi, Ming Li, Yue-Jin Liu, Ming-Hua Zeng
Organic letters 2021 Sep 17A 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.
Mao-Gui Huang, Shuai Shi, Ming Li, Yue-Jin Liu, Ming-Hua Zeng. Salicylaldehyde-Promoted Cobalt-Catalyzed C-H/N-H Annulation of Indolyl Amides with Alkynes: Direct Synthesis of a 5-HT3 Receptor Antagonist Analogue. Organic letters. 2021 Sep 17;23(18):7094-7099
PMID: 34449224
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