Abstract

A copper catalyzed controllable α-chlorination of nafimidone derivatives with HCl was achieved. This green and efficient catalysis proceeds via a ligand to metal charge transfer (LMCT) process and used air as a green oxidant. With different reaction conditions, the chlorinated or dichlorinated nafimidone derivatives could be controllable synthesized in good to excellent yields with a high functional group tolerance and a broad substrate scope. This controllable and practical strategy provides access to potentially bioactive nafimidone derivatives.

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