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可调节的[3+2]和[4+2]环加成反应合成吡咯烷和哌啶。

Tunable [3+2] and [4+2] annulations for pyrrolidine and piperidine synthesis.

机构信息

Department of Chemistry and Biochemistry and School of Green Chemistry and Engineering, The University of Toledo, Toledo, Ohio 43606, USA.

出版信息

Chem Commun (Camb). 2023 May 23;59(42):6418-6421. doi: 10.1039/d3cc01400b.

Abstract

N-heterocycles are privileged pharmaceutical scaffolds in drug discovery and development. We disclose here divergent intermolecular coupling strategies that can access diverse N-heterocycles directly from olefins. The radical-to-polar mechanistic switching is key for the divergent cyclization processes. These distinctive annulations result in the coupling of alkenes with simple bifunctional reagents for divergent N-heterocycle syntheses.

摘要

杂环是药物发现和开发中的重要药物骨架。我们在这里公开了不同的分子间偶联策略,可以直接从烯烃中获得不同的杂环。自由基到极性的机理转换是发散环化过程的关键。这些独特的环化反应导致烯烃与简单双功能试剂的偶联,从而实现杂环的发散合成。

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本文引用的文献

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