Highly Regioselective Synthesis of 2-Acylindolines through Cobalt-Catalyzed C−H Activation/[3+2] Annulation of Aniline Derivatives and Acrylates,Advanced Synthesis & Catalysis

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Highly Regioselective Synthesis of 2-Acylindolines through Cobalt-Catalyzed C−H Activation/[3+2] Annulation of Aniline Derivatives and Acrylates
Advanced Synthesis & Catalysis ( IF 4.4 ) Pub Date : 2022-11-14 , DOI: 10.1002/adsc.202200965
Xun Tian ₁ , Ailin Pan ₁ , Ya Du ₁ , Lening Zhang ₁ , Cuirong Qin ₁ , Shengzu Duan ₂ , Lijuan Yang ₃ , Xiaodong Yang ₁

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An approach for 2-acyl indolines synthesis through Cobalt-catalyzed C−H activation/[3+2] annulation of aniline derivatives and acrylates is described. The method employs cobalt catalyst to afford a wide variety of functionalized 2-acylindolines with high regioselectivity. The mechanism is investigated by KIE experiments and deuterium-labeling experiment. The gram-scale synthesis and synthetic transformations are also conducted, confirming the scalability and application value.

中文翻译：

通过钴催化的 C−H 活化/苯胺衍生物和丙烯酸酯的 [3+2] 环化高区域选择性合成 2-酰基二氢萘

描述了一种通过钴催化的苯胺衍生物和丙烯酸酯的 C−H 活化/[3+2] 环化合成 2-酰基二氢吲哚的方法。该方法使用钴催化剂来提供各种具有高区域选择性的功能化 2-酰基二氢吲哚。通过KIE实验和氘标记实验研究了该机制。还进行了克级合成和合成转化，证实了可扩展性和应用价值。

更新日期：2022-11-14

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