Domino Carbopalladation/C–H Activation as a Quick Access to Polycyclic Frameworks,Organic Letters

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Domino Carbopalladation/C–H Activation as a Quick Access to Polycyclic Frameworks
Organic Letters ( IF 4.9 ) Pub Date : 2018-01-10 00:00:00 , DOI: 10.1021/acs.orglett.7b03843
Nemai Saha _{1,

2} , Haiwen Wang ₁ , Shengyi Zhang ₁ , Yongliang Du ₁ , Daqian Zhu ₁ , Yumin Hu ₁ , Peng Huang _{1,

2} , Shijun Wen _{1,

2}

Affiliation

A new type of domino reaction for synthesis of heterocycles fusing the important bioactive cores, such as oxindole, indoline, and isoquinoline, is presented. Upon exposure to the very common palladium catalyst, the conceptually designed N-alkenyl iodobiaryls undergo a sequential carbopalladation/C–H activation to build polycyclic frameworks. These novel unique frameworks may provide structure sources in fragment-based drug discovery.

中文翻译：

Domino Carbopalladation / CH激活作为对多环框架的快速访问

提出了一种新型的多米诺骨牌反应，用于合成重要的生物活性核心，如羟吲哚，吲哚啉和异喹啉，以合成杂环。暴露于非常常见的钯催化剂后，概念设计的N-烯基碘联二芳基化合物经历了顺序的碳钯/ CH活化，从而建立了多环骨架。这些新颖独特的框架可以为基于片段的药物发现提供结构来源。

更新日期：2018-01-10

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