Abstract

AbstractRegioselective halogenation of heteroaromatics via C−H activation is a challenge in organic synthesis. In this paper, we described a simple, mild and highly selective protocol for halogenating C‐5 of N‐(8‐quinolinyl) amides with cuprous halides in the presence of NFSI (N‐Fluorobenzenesulfonimide) at room temperature. The different chloro‐, bromo‐ and iodo‐ substituted N‐(8‐quinolinyl) amides on C‐5 position were obtained respectively in good yields with excellent substrates tolerance.

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