Cobalt-Catalyzed Halogen-Retentive C–H Activation and Its Application in Medicinal Chemistry

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.