Herein, we report the in situ-generated transient bromoiodane-mediated brominative annulation of 2-alkynyl arylimidate for the synthesis of 4-bromoisoquinolines at room temperature. Using a simple hypervalent iodine reagent PIDA as a mild oxidant and potassium bromide as the halogen source, a broad range of valuable 4-bromoisoquinolines can be synthesized in excellent yields. The reaction features readily available chemicals, mild metal-free conditions, and high functional group tolerance, providing an efficient alternative for the construction of halogenated isoquinolines.

中文翻译：

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使用原位生成的瞬时溴碘化通过 2-炔基芳基酯的溴化环化无金属合成 4-溴异喹啉


在此，我们报道了原位产生的瞬时溴碘介导的 2-炔基芳基丙烯酸酯的溴化环化，用于在室温下合成 4-溴异喹啉。使用简单的高价碘试剂 PIDA 作为温和氧化剂，溴化钾作为卤素源，可以以极高的产率合成多种有价值的 4-溴异喹啉。该反应具有易得化学品、温和的无金属条件和高官能团耐受性，为构建卤代异喹啉提供了一种有效的替代方案。