Cobalt-Catalyzed Halogen-Retentive C-H Activation and Its Application in Medicinal Chemistry
Yongke Lei1, Xiyu Luo1, Lutz Ackermann2
1Guangxi Key Laboratory of Bioactive Molecules Research and Evaluation, School of Pharmacy, Guangxi Medical University, Nanning 530021, China.
Abstract:
The development of C-C bond-forming strategies that retain the halogen atom represents an attractive yet challenging endeavor in synthetic chemistry, offering unique opportunities for downstream diversification. Herein, we report the halogen-retentive C-H annulation of haloalkynes, particularly bromoalkynes, enabled by an earth-abundant cobalt catalyst. The retained bromine atom serves as a versatile linchpin for subsequent C-H activation reactions, providing a general synthetic route for potential bioactive molecules and identifying a new compound with anti-cancer activity.
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