Recent Advances in the Regioselective Synthesis of Indoles via C-H Activation/Functionalization
Recent Advances in the Regioselective Synthesis of Indoles via C-H Activation/Functionalization
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DOI：
10.1055/s-0037-1609733
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发表时间：
2018-07-01
影响因子：
2.6
通讯作者：
Sharma, Upendra
中科院分区：
文献类型：
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作者：
Kumar, Inder;Kumar, Rakesh;Sharma, Upendra
吲哚是一种重要的杂环基序，广泛存在于生物活性天然产物和药物中。从Fisher吲哚合成到最近开发的基于C-H活化/官能化的方法，已经投入了大量的努力来合成吲哚。本文综述了2010年以来吲哚类化合物（包括2-取代、3-取代和2，3-二取代吲哚）的区域选择性合成研究进展。1引言2金属催化合成2-取代吲哚3金属催化合成3-取代吲哚4无金属合成3-取代吲哚5金属催化2，3-二取代吲哚合成5.1金属催化分子内2，3-二取代吲哚合成5.2金属催化分子间2，3-二取代吲哚合成6无金属2，3-二取代吲哚合成3-二取代吲哚的合成6.1 N-保护的2，3-二取代吲哚的合成6.2 N-不保护的2，3-二取代吲哚的合成7应用8总结与展望
Indole is an important heterocyclic motif that occurs ubiquitously in bioactive natural products and pharmaceuticals. Immense efforts have been devoted to the synthesis of indoles starting from the Fisher indole synthesis to the recently developed C-H activation/functionalization-based methods. Herein, we have reviewed the progress made on the regioselective synthesis of functionalized indoles, including 2-substituted, 3-substituted and 2,3-disusbstituted indoles, since the year 2010. 1 Introduction 2 Metal-Catalyzed Synthesis of 2-Substituted Indoles 3 Metal-Catalyzed Synthesis of 3-Substituted Indoles 4 Metal-Free Synthesis of 3-Substituted Indoles 5 Metal-Catalyzed 2,3-Disubstituted Indole Synthesis 5.1 Metal-Catalyzed Intramolecular 2,3-Disubstituted Indole Synthesis 5.2 Metal-Catalyzed Intermolecular 2,3-Disubstituted Indole Synthesis 6 Metal-Free 2,3-Disubstituted Indole Synthesis 6.1 N-Protected 2,3-Disubstituted Indole Synthesis 6.2 N-Unprotected 2,3-Disubstituted Indole Synthesis 7 Applications 8 Summary and Outlook