Described herein is the discovery of a palladium‐catalyzed chlorocylization strategy for the synthesis of 3‑chloroindoles tolerated with a wide range of functional groups in moderate to excellent yields. In this transformation, the solvent effect is so important that only THF presents the positive effect. Furthermore, the present method provides an essay access to the N‐unprotected 3‐chloroindoles. A mechanism study showed that 2‐alkynlanilines were catalyzed by palladium to from corresponding indoles, followed by copper‐mediated oxidation chlorination to deliver the 3‐chloroindoles products.

中文翻译：

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通过钯催化未掩蔽的 2-炔基苯胺的氯环化合成 3-氯吲哚


本文描述了一种钯催化的叶基化策略，用于合成 3-氯吲哚，该 3-氯吲哚具有多种官能团耐受性，产率中等至极高。在这个转化中，溶剂效应非常重要，以至于只有 THF 才具有积极效应。此外，该方法提供了一篇对 N-未受保护的 3-氯吲哚的论文访问。一项机制研究表明，2-炔基苯胺被钯催化从相应的吲哚中得到，然后是铜介导的氧化氯化反应，以得到 3-氯吲哚产物。